GSK-1070916 (Synonyms: GSK-1070916A)

目录号: HY-70044 纯度: 99.54%: Data Sheet SDS COA 产品使用指南
FAQs
技术支持

GSK-1070916 是有效，选择性，ATP 竞争型的极光激酶 B/C (aurora B/C) 抑制剂，K_i 值分别为 0.38 和 1.5 nM。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

GSK-1070916 Chemical Structure

CAS No. : 942918-07-2

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1101	In-stock
1 mg	￥439	In-stock
5 mg	￥986	In-stock
10 mg	￥1596	In-stock
25 mg	￥2364	In-stock
50 mg	￥3348	In-stock
100 mg	￥4956	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of GSK-1070916:

GSK-1070916 (GMP) 询价

MCE 顾客使用本产品发表的 6 篇科研文献

GSK-1070916 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型

Aurora Kinase Aurora A Aurora B Aurora C

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with K_is of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.

IC₅₀ & Target^[1]

Aurora B

0.38 nM (Ki)

Aurora C

1.5 nM (Ki)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
786-0	EC₅₀	57 nM Compound: GSK 1070916	Antiproliferative activity against human 786-0 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human 786-0 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
A2780	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human A2780 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human A2780 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
A375P	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human A375P cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human A375P cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
A498	EC₅₀	33 nM Compound: GSK 1070916	Antiproliferative activity against human A498 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human A498 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
A549	EC₅₀	7 nM Compound: 17k, GSK-1070916	Antiproliferative activity against human A549 cells after 6 to 7 days by celltiter-glo luminescence assay in absence of 70% human serum albumin Antiproliferative activity against human A549 cells after 6 to 7 days by celltiter-glo luminescence assay in absence of 70% human serum albumin	[PMID: 20420387]
A549	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human A549 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human A549 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
A549	EC₅₀	7 nM Compound: GSK-1070916	Cytotoxicity against human A549 cells in presence of 10% human serum Cytotoxicity against human A549 cells in presence of 10% human serum	[PMID: 20335034]
ARH-77	EC₅₀	15 nM Compound: GSK 1070916	Antiproliferative activity against human ARH-77 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human ARH-77 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
ASPC1	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
BC-3	EC₅₀	27 nM Compound: GSK 1070916	Antiproliferative activity against human BC-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human BC-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
BV-173	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human BV-173 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human BV-173 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
BXPC-3	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CA46	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human CA46 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CA46 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CCRF-CEM	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human CCRF-CEM cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CCRF-CEM cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CCRF-HSB-2	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human HSB-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HSB-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CCRF-SB	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human CCRF-SB cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CCRF-SB cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CESS	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human CESS cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CESS cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CMK	EC₅₀	27 nM Compound: GSK 1070916	Antiproliferative activity against human CMK cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CMK cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
COLO 201	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human COLO201 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human COLO201 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
COLO 205	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human COLO 205 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human COLO 205 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
COLO 320DM	EC₅₀	96 nM Compound: GSK 1070916	Antiproliferative activity against human COLO 320DM cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human COLO 320DM cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
COLO-320-HSR	EC₅₀	92 nM Compound: GSK 1070916	Antiproliferative activity against human COLO 320HSR cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human COLO 320HSR cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CRO-AP2	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human CRO-AP2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CRO-AP2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CTV-1	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human CTV-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CTV-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
DB	EC₅₀	11 nM Compound: GSK 1070916	Antiproliferative activity against human DB cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human DB cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
DG-75	EC₅₀	18 nM Compound: GSK 1070916	Antiproliferative activity against human DG-75 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human DG-75 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
DLD-1	EC₅₀	28 nM Compound: GSK 1070916	Antiproliferative activity against human DLD-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human DLD-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
DOHH-2	EC₅₀	14 nM Compound: GSK 1070916	Antiproliferative activity against human DOHH-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human DOHH-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
DU-145	EC₅₀	15 nM Compound: GSK 1070916	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human DU-145 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Daudi	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human Daudi cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Daudi cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
EB-3	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human EB-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human EB-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
EB2	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human EB2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human EB2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
EM-2	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human EM-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human EM-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Farage	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human Farage cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Farage cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
GA-10	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human GA-10 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human GA-10 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
GDM-1	EC₅₀	21 nM Compound: GSK 1070916	Antiproliferative activity against human GDM-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human GDM-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HCT-116	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HCT-8	EC₅₀	38 nM Compound: GSK 1070916	Antiproliferative activity against human HCT-8 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HCT-8 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HD-MY-Z	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human HD-MY-Z cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HD-MY-Z cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HEL 92.1.7	EC₅₀	60 nM Compound: GSK 1070916	Antiproliferative activity against human HEL 92.1.7 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HEL 92.1.7 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HH	EC₅₀	18 nM Compound: GSK 1070916	Antiproliferative activity against human HH cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HH cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HL-60	EC₅₀	10 nM Compound: GSK 1070916	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HN5	EC₅₀	10 nM Compound: GSK 1070916	Antiproliferative activity against human HN5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HN5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HT	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human HT cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HT cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HT-29	EC₅₀	10 nM Compound: GSK 1070916	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HUVEC	EC₅₀	3900 nM Compound: GSK 1070916	Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 6 days by cell titer glo assay Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 6 days by cell titer glo assay	[PMID: 19567821]
HeLa	EC₅₀	13 nM Compound: GSK 1070916	Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Hep 3B2	EC₅₀	12 nM Compound: GSK 1070916	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HuT78	EC₅₀	14 nM Compound: GSK 1070916	Antiproliferative activity against human HuT78 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HuT78 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
J-RT3-T3-5	EC₅₀	9 nM Compound: GSK 1070916	Antiproliferative activity against human J-RT3-T3-5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human J-RT3-T3-5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
JIYOYE	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human JIYOYE cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human JIYOYE cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
JM1	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human JM1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human JM1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
JVM-3	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human JVM-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human JVM-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Jurkat	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
K562	EC₅₀	13 nM Compound: GSK 1070916	Antiproliferative activity against human K562 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human K562 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
KCL-22	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human KCL-22 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human KCL-22 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
KG-1	EC₅₀	32 nM Compound: GSK 1070916	Antiproliferative activity against human KG-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human KG-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
L-428	EC₅₀	31 nM Compound: GSK 1070916	Antiproliferative activity against human L-428 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human L-428 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
LNCaP	EC₅₀	12 nM Compound: GSK 1070916	Antiproliferative activity against human LNCaP cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human LNCaP cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
LoVo	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human LoVo cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human LoVo cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MC-CAR	EC₅₀	9 nM Compound: GSK 1070916	Antiproliferative activity against human MC-CAR cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MC-CAR cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MC116	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human MC116 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MC116 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MCF7	EC₅₀	13 nM Compound: GSK 1070916	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MDA-MB-231	EC₅₀	11 nM Compound: GSK 1070916	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MDA-MB-453	EC₅₀	6 nM Compound: GSK 1070916	Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MDA-MB-468	EC₅₀	12 nM Compound: GSK 1070916	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MEG-01	EC₅₀	44 nM Compound: GSK 1070916	Antiproliferative activity against human MEG-01 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MEG-01 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MHH-PREB-1	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human MHH-PREB-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MHH-PREB-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MIA PaCa-2	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human Mia PaCa cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Mia PaCa cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
ML-2	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human ML-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human ML-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MOLT-16	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human MOLT-16 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MOLT-16 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MOLT-3	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human MOLT-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MOLT-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MOLT-4	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MV4-11	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MX1	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human MX1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MX1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NALM-6	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human NALM-6 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NALM-6 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NAMALVA	EC₅₀	6 nM Compound: GSK 1070916	Antiproliferative activity against human NAMALWA cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NAMALWA cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NB-4	EC₅₀	11 nM Compound: GSK 1070916	Antiproliferative activity against human NB4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NB4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NC-37	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human NC-37 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NC-37 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NCI-H1155	EC₅₀	40 nM Compound: GSK 1070916	Antiproliferative activity against human NCI-H1155 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NCI-H1155 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NCI-H1299	EC₅₀	23 nM Compound: GSK 1070916	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NCI-H157	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human NCI-H157 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NCI-H157 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NCI-H358	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human NCI-H358 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NCI-H358 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NCI-H460	EC₅₀	14 nM Compound: GSK 1070916	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NCI-H630	EC₅₀	127 nM Compound: GSK 1070916	Antiproliferative activity against human NCI-H630 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NCI-H630 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NOMO-1	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human NOMO-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NOMO-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NU-DUL-1	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human NU-DUL-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NU-DUL-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
OCI-AML-3	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human OCI-AML-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human OCI-AML-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
OCI-AML2	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human OCI-AML2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human OCI-AML2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
OCI-LY19	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human OCILY19 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human OCILY19 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
OVCAR-3	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
OVCAR-4	EC₅₀	11 nM Compound: GSK 1070916	Antiproliferative activity against human OVCAR-4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human OVCAR-4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
OVCAR-8	EC₅₀	30 nM Compound: GSK 1070916	Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
P3HR-1	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human P3HR-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human P3HR-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
PANC-1	EC₅₀	13 nM Compound: GSK 1070916	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
PC-3	EC₅₀	11 nM Compound: GSK 1070916	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Pfeiffer	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human Pfeiffer cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Pfeiffer cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
RCK8	EC₅₀	38 nM Compound: GSK 1070916	Antiproliferative activity against human RCK8 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human RCK8 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
RKO	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human RKO cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human RKO cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
RL	EC₅₀	10 nM Compound: GSK 1070916	Antiproliferative activity against human RL cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human RL cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
RPMI-6666	EC₅₀	10 nM Compound: GSK 1070916	Antiproliferative activity against human RPMI-6666 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human RPMI-6666 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
RPMI-8226	EC₅₀	111 nM Compound: GSK 1070916	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Raji	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human Raji cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Raji cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Rec1	EC₅₀	77 nM Compound: GSK 1070916	Antiproliferative activity against human REC1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human REC1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SEM	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human SEM cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SEM cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SK-BR-3	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SK-MEL-2	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human SK-MEL-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SK-MEL-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SK-MEL-28	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human SK-MEL-28 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SK-MEL-28 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SK-MEL-5	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human SK-MEL-5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SK-MEL-5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SK-OV-3	EC₅₀	12 nM Compound: GSK 1070916	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SR	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human SR cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SR cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
ST486	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human ST486 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human ST486 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SU-DHL-16	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human SU-DHL-16 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SU-DHL-16 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SU-DHL-5	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human SU-DHL-5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SU-DHL-5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SU-DHL-6	EC₅₀	6 nM Compound: GSK 1070916	Antiproliferative activity against human SU-DHL-6 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SU-DHL-6 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SU-DHL10	EC₅₀	15 nM Compound: GSK 1070916	Antiproliferative activity against human SU-DHL-10 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SU-DHL-10 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SUD4	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human SU-DHL-4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SU-DHL-4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SUP-B15	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human SUP-B15 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SUP-B15 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SW 954	EC₅₀	11 nM Compound: GSK 1070916	Antiproliferative activity against human SW 954 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SW 954 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SW-620	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human SW620 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SW620 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SW1417	EC₅₀	19 nM Compound: GSK 1070916	Antiproliferative activity against human SW1417 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SW1417 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SW48	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human SW48 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SW48 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SW480	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human SW480 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SW480 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
T47D	EC₅₀	13 nM Compound: GSK 1070916	Antiproliferative activity against human T47D cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human T47D cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
THP-1	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Toledo	EC₅₀	15 nM Compound: GSK 1070916	Antiproliferative activity against human Toledo cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Toledo cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
U-266	EC₅₀	422 nM Compound: GSK 1070916	Antiproliferative activity against human U266B1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human U266B1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
U-937	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human U-937 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human U-937 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
U2OS	EC₅₀	34 nM Compound: GSK 1070916	Antiproliferative activity against human U2OS cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human U2OS cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
WiDr	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human WiDr cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human WiDr cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]

体外研究
(In Vitro)

GSK-1070916 强效抑制 Aurora B/INCENP 和 Aurora C/INCENP 激酶，K_i 分别为 0.38 和 1.45 nM，但对 Aurora A/TPX2 的抑制作用较弱，K_i 为 492 nM。GSK-1070916 还能抑制 FLT1、TIE2、SIK、FLT4 和 FGFR1，IC₅₀ 值分别为 42、59、70、74 和 78 nM。GSK-1070916 处理 A549 人肺癌细胞可产生强效的抗增殖作用 (EC₅₀=7 nM)^[1]。
GSK-1070916 可抑制一组肿瘤细胞系，并显示出可抑制所有细胞系中 HH3-S10 的磷酸化，平均 EC₅₀ 值范围为 8 至 118 nM^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

在植入人结肠肿瘤 (HCT116) 异种移植瘤的裸鼠中，单剂量腹腔注射 GSK-1070916 可剂量依赖性地抑制 HH3-S10 磷酸化。重复腹腔注射 GSK-1070916 对 8 种肿瘤类型中的 4 种 (肺癌，A549；结肠癌，HCT116；急性髓性白血病 (AML)，HL60；以及慢性髓性白血病，K562) 产生完全或部分抗肿瘤活性，对 8 种肿瘤类型中的 3 种 (结肠癌，Colo205；肺癌，H460；以及乳腺癌，MCF-7) 产生稳定效果，并对 8 种肿瘤类型中的 1 种 (结肠癌，SW620) 产生肿瘤生长延缓。每日服用 GSK-1070916 通常耐受性良好^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

507.63

Formula

C₃₀H₃₃N₇O

CAS 号

942918-07-2

性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 16.67 mg/mL (32.84 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9699 mL	9.8497 mL	19.6994 mL
5 mM	0.3940 mL	1.9699 mL	3.9399 mL
10 mM	0.1970 mL	0.9850 mL	1.9699 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (3.29 mM); 澄清溶液

此方案可获得 ≥ 1.67 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (3.29 mM); 澄清溶液

此方案可获得 ≥ 1.67 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 1 mg/mL (1.97 mM); 澄清溶液

此方案可获得 ≥ 1 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.55%

选择批次：

Data Sheet (646 KB) SDS (393 KB)

COA (286 KB) HNMR (185 KB) LCMS (469 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Adams ND, et al. Discovery of GSK-1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001. [Content Brief]

[2]. Hardwicke MA, et al. GSK-1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models. Mol Cancer Ther. 2009 Jul;8(7):1808-17. [Content Brief]

Cell Assay ^[2]	A panel of tumor cell lines are plated in 96-well plates in the recommended growth media and incubated at 37°C in 5% CO₂ overnight. The following day, the cells are treated with serial dilutions of GSK-1070916. At this time, one set of cells is treated with CellTiter-Glo for a time equal to 0 (T=0) measurement. Following a 6- to 7-d incubation with compound, cell proliferation is measured using the CellTiter-Glo reagent^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice: Tumors are initiated by injection of tumor cell suspensions (A549, SW620, HCT116, H460, MCF-7, HL60, K562) or tumor fragments (Colo205) s.c. into nude (A549, SW620, HCT116, H460, MCF-7, HL60, and Colo205) or severe combined immunodeficient (SCID; K562) mice. When the tumors reach a volume of 80 to 200 mm³, the mice are randomized into groups of 5 to 10 mice per group. GSK-1070916 is administered at 25, 50, or 100 mg/kg once daily for 5 consecutive days-on, 2d-off, schedule for two (Colo205 and HL60) or three (A549, SW620, HCT116, H460, MCF-7, K562) cycles. Tumors are measured twice weekly^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Adams ND, et al. Discovery of GSK-1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001. [Content Brief] [2]. Hardwicke MA, et al. GSK-1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models. Mol Cancer Ther. 2009 Jul;8(7):1808-17. [Content Brief]

GSK-1070916 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9699 mL	9.8497 mL	19.6994 mL	49.2485 mL
	5 mM	0.3940 mL	1.9699 mL	3.9399 mL	9.8497 mL
	10 mM	0.1970 mL	0.9850 mL	1.9699 mL	4.9248 mL
	15 mM	0.1313 mL	0.6566 mL	1.3133 mL	3.2832 mL
	20 mM	0.0985 mL	0.4925 mL	0.9850 mL	2.4624 mL
	25 mM	0.0788 mL	0.3940 mL	0.7880 mL	1.9699 mL
	30 mM	0.0657 mL	0.3283 mL	0.6566 mL	1.6416 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK-1070916942918-07-2GSK-1070916AGSK1070916GSK 1070916Aurora KinaseApoptosisInhibitorinhibitorinhibit

产品名称：			* 需求量：
* 客户姓名：			* Email：
* 电话：			* 公司或机构名称：
留言给我们：

产品名称：			* Lot #：
* 客户姓名：			* Email：
电话：			* 部门：
* 公司或机构名称：
留言给我们：

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。	站点地图隐私声明
沪ICP备15051369号-4 上海工商沪公网安备31011502019417 沪(浦)应急管危经许[2021]201709(QFYS) 营业执照（三证合一）
Copyright © 2013-2025 MedChemExpress. All Rights Reserved.

GSK-1070916 (Synonyms: GSK-1070916A)

Customer Review

Other Forms of GSK-1070916:

MCE 顾客使用本产品发表的 6 篇科研文献

GSK-1070916 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Aurora Kinase 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

GSK-1070916 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

姓名
邮箱 *

Sorry, but the email address you supplied was invalid.

GSK-1070916 (Synonyms: GSK-1070916A)

Customer Review

Other Forms of GSK-1070916:

GSK-1070916 相关抗体

MCE 顾客使用本产品发表的 6 篇科研文献

GSK-1070916 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Aurora Kinase 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

GSK-1070916 相关抗体:

摩尔计算器

稀释计算器

GSK-1070916 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

Request for HNMR Report

Request for HNMR Report

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z