Mocetinostat (Synonyms: MGCD0103)

目录号: HY-12164 纯度: 99.13%: Data Sheet SDS COA 产品使用指南
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Mocetinostat (MGCD0103)是一种有效，可口服和同种型选择性的 HDAC (Class I/IV) 抑制剂，抑制HDAC1，HDAC2，HDAC3 和 HDAC11 的IC₅₀分别为0.15，0.29，1.66 和 0.59 μM。 Mocetinostat对HDAC4，HDAC5，HDAC6，HDAC7或HDAC8没有抑制作用。

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Mocetinostat Chemical Structure

CAS No. : 726169-73-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥698	In-stock
1 mg	￥363	In-stock
5 mg	￥800	In-stock
10 mg	￥1100	In-stock
25 mg	￥1900	In-stock
50 mg	￥2700	In-stock
100 mg	￥4300	In-stock
200 mg	现货	询价
500 mg	现货	询价
1 g		询价
5 g		询价

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Customer Review

Other Forms of Mocetinostat:

Mocetinostat (Standard) 询价

MCE 顾客使用本产品发表的 21 篇科研文献

Mocetinostat 相关产品

•相关化合物库:

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•同靶点蛋白产品:

查看 HDAC 亚型特异性产品:

查看所有亚型

HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Mocetinostat (MGCD0103) is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC₅₀s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8.

IC₅₀ & Target^[1]

HDAC1

0.15 μM (IC₅₀)

HDAC2

0.29 μM (IC₅₀)

HDAC11

0.59 μM (IC₅₀)

HDAC3

1.66 μM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.9 μM Compound: 8, MGCD0103	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 18570366]
A549	IC₅₀	1.279 μM Compound: MGCD0103	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 23206867]
A549	IC₅₀	1.65 μM Compound: MGCD0103	Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 24095018]
A549	IC₅₀	1.73 μM Compound: MGCD0103, Mocetinostat	Cytotoxicity against human A549 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay Cytotoxicity against human A549 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay	[PMID: 23829483]
A549	IC₅₀	11.87 μM Compound: MGCD0103	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	10.1039/C5MD00247H
A549	IC₅₀	1275 nM Compound: 4; MGCD0103	Antiproliferative activity against human A549 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
A549	IC₅₀	14.57 μM Compound: MGCD0103	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay	10.1039/C5MD00247H
A549	IC₅₀	2.08 μM Compound: Mocetinostat	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
A549	IC₅₀	59.9 μM Compound: MGCD0103	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00247H
CAKI-1	IC₅₀	265 nM Compound: 4; MGCD0103	Antiproliferative activity against human CAKI-1 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human CAKI-1 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
CT26	GI₅₀	1.77 μM Compound: 4; MGCD-0103	Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK-8 assay Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK-8 assay	[PMID: 35390714]
CT26	GI₅₀	1.8 μM Compound: 9; MGCD-0103	Antiproliferative activity against mouse CT26 cells measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse CT26 cells measured after 72 hrs by CCK8 assay	[PMID: 34783558]
DOHH-2	IC₅₀	74 nM Compound: 4; MGCD0103	Antiproliferative activity against human DOHH-2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human DOHH-2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
DU-145	IC₅₀	0.67 μM Compound: 8, MGCD0103	Antiproliferative activity against human Du145 cells after 72 hrs by MTT assay Antiproliferative activity against human Du145 cells after 72 hrs by MTT assay	[PMID: 18570366]
DU-145	IC₅₀	2.06 μM Compound: MGCD0103, Mocetinostat	Cytotoxicity against human DU145 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay Cytotoxicity against human DU145 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay	[PMID: 23829483]
ES-2	IC₅₀	25 nM Compound: 4; MGCD0103	Antiproliferative activity against human ES2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ES2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
HCT-116	EC₅₀	0.45 μM Compound: 8, MGCD0103	Induction of p21cip/waf1 protein expression in human HCT116 cells relative to MS275 Induction of p21cip/waf1 protein expression in human HCT116 cells relative to MS275	[PMID: 18570366]
HCT-116	EC₅₀	0.6 μM Compound: A, MGCD0103	Induction of p21WAF1/CIP1 expression in human HCT116 cells assessed as tubulin level after 16 hrs by luciferase assay Induction of p21WAF1/CIP1 expression in human HCT116 cells assessed as tubulin level after 16 hrs by luciferase assay	[PMID: 19114304]
HCT-116	EC₅₀	< 1 μM Compound: 8, MGCD0103	Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase	[PMID: 18570366]
HCT-116	IC₅₀	0.29 μM Compound: 8, MGCD0103	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 18570366]
HCT-116	IC₅₀	0.3 μM Compound: A, MGCD0103	Antiproliferative activity against human HCT116 cells by MTT assay Antiproliferative activity against human HCT116 cells by MTT assay	[PMID: 19114304]
HCT-116	IC₅₀	0.31 μM Compound: 4, MGCD-0103	Antiproliferative activity against human HCT116 cells Antiproliferative activity against human HCT116 cells	[PMID: 21742496]
HCT-116	IC₅₀	0.327 μM Compound: MGCD0103	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 23206867]
HCT-116	IC₅₀	0.396 μM Compound: Mocetinostat	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
HCT-116	IC₅₀	0.53 μM Compound: 4; MGCD0103	Antiproliferative activity against human HCT-116 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
HCT-116	IC₅₀	0.7 μM Compound: MGCD0103, Mocetinostat	Cytotoxicity against human HCT116 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay Cytotoxicity against human HCT116 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay	[PMID: 23829483]
HCT-116	IC₅₀	1.24 μM Compound: MGCD0103	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	10.1039/C5MD00247H
HCT-116	IC₅₀	1.57 μM Compound: MGCD0103	Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 24095018]
HCT-116	IC₅₀	29.69 μM Compound: MGCD0103	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00247H
HCT-116	IC₅₀	3.51 μM Compound: MGCD0103	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay	10.1039/C5MD00247H
HCT-116	IC₅₀	310 nM Compound: 5, MGCD0103	Antiproliferative activity against human HCT116 cells assessed as growth inhibition Antiproliferative activity against human HCT116 cells assessed as growth inhibition	[PMID: 21650221]
HEK293	IC₅₀	130 nM Compound: MGCD-0103	Inhibition of HDAC1 in HEK293 cells Inhibition of HDAC1 in HEK293 cells	[PMID: 18308563]
HEK293	IC₅₀	1338 nM Compound: 4; MGCD0103	Antiproliferative activity against human HEK293 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HEK293 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
HEK293	IC₅₀	610 nM Compound: MGCD-0103	Inhibition of HDAC3 in HEK293 cells Inhibition of HDAC3 in HEK293 cells	[PMID: 18308563]
HL-60	IC₅₀	0.418 μM Compound: MGCD0103	Antiproliferative activity against human HL-60 cells incubated for 48 hrs Antiproliferative activity against human HL-60 cells incubated for 48 hrs	[PMID: 36549114]
HMEC	IC₅₀	20 μM Compound: 8, MGCD0103	Antiproliferative activity against HMEC after 72 hrs by MTT assay Antiproliferative activity against HMEC after 72 hrs by MTT assay	[PMID: 18570366]
HMEC	IC₅₀	21 μM Compound: A, MGCD0103	Antiproliferative activity against HMEC by MTT assay Antiproliferative activity against HMEC by MTT assay	[PMID: 19114304]
HeLa	IC₅₀	3.32 μM Compound: MGCD0103	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay	10.1039/C5MD00247H
HeLa	IC₅₀	3.42 μM Compound: MGCD0103	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay	10.1039/C5MD00247H
HeLa	IC₅₀	43.8 μM Compound: MGCD0103	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00247H
HeLa	IC₅₀	660 nM Compound: 4; MGCD0103	Antiproliferative activity against human HeLa cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
Hep 3B2	IC₅₀	0.823 μM Compound: Mocetinostat	Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
HepG2	IC₅₀	0.876 μM Compound: Mocetinostat	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
HepG2	IC₅₀	4.05 μM Compound: MGCD0103	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay	10.1039/C5MD00247H
HepG2	IC₅₀	4.25 μM Compound: MGCD0103	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	10.1039/C5MD00247H
HepG2	IC₅₀	5.79 μM Compound: MGCD0103	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00247H
Jurkat	IC₅₀	150 nM Compound: 4; MGCD0103	Antiproliferative activity against human Jurkat cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Jurkat cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
K562	IC₅₀	322 nM Compound: 4; MGCD0103	Antiproliferative activity against human K562 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
KARPAS-299	IC₅₀	4.15 μM Compound: MGCD0103	Antiproliferative activity against human KARPAS-299 cells incubated for 48 hrs Antiproliferative activity against human KARPAS-299 cells incubated for 48 hrs	[PMID: 36549114]
Kasumi 1	IC₅₀	0.151 μM Compound: MGCD0103	Antiproliferative activity against human Kasumi 1 cells incubated for 48 hrs Antiproliferative activity against human Kasumi 1 cells incubated for 48 hrs	[PMID: 36549114]
MC-38	GI₅₀	1.64 μM Compound: 4; MGCD-0103	Antiproliferative activity against mouse MC38 cells after 72 hrs by CCK-8 assay Antiproliferative activity against mouse MC38 cells after 72 hrs by CCK-8 assay	[PMID: 35390714]
MC-38	GI₅₀	21 μM Compound: 9; MGCD-0103	Antiproliferative activity against mouse MC38 cells measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse MC38 cells measured after 72 hrs by CCK8 assay	[PMID: 34783558]
MC-38	IC₅₀	1.84 μM Compound: 4; MGCD0103	Antiproliferative activity against mouse MC38 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse MC38 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
MCF7	IC₅₀	1.26 μM Compound: MGCD0103, Mocetinostat	Cytotoxicity against human MCF7 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay Cytotoxicity against human MCF7 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay	[PMID: 23829483]
MCF7	IC₅₀	2.49 μM Compound: MGCD0103	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	10.1039/C5MD00247H
MCF7	IC₅₀	4.807 μM Compound: MGCD0103	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 23206867]
MCF7	IC₅₀	56.81 μM Compound: MGCD0103	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	10.1039/C5MD00247H
MCF7	IC₅₀	84.17 μM Compound: MGCD0103	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00247H
MDA-MB-231	IC₅₀	309 nM Compound: 4; MGCD0103	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
MHCC97H	IC₅₀	4.563 μM Compound: Mocetinostat	Cytotoxicity against human MHCC97H cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MHCC97H cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
MIA PaCa-2	IC₅₀	303 nM Compound: 4; MGCD0103	Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
MKN-45	IC₅₀	0.61 μM Compound: Mocetinostat	Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
MV4-11	IC₅₀	0.19 μM Compound: MGCD0103	Antiproliferative activity against human MV4-11 cells incubated for 48 hrs Antiproliferative activity against human MV4-11 cells incubated for 48 hrs	[PMID: 36549114]
NB-4	IC₅₀	0.406 μM Compound: MGCD0103	Antiproliferative activity against human NB4 cells incubated for 48 hrs Antiproliferative activity against human NB4 cells incubated for 48 hrs	[PMID: 36549114]
NCI-H1299	IC₅₀	1440 nM Compound: 5, MGCD0103	Antiproliferative activity against human H1299 cells Antiproliferative activity against human H1299 cells	[PMID: 21650221]
NCI-N87	IC₅₀	606 nM Compound: 4; MGCD0103	Antiproliferative activity against human NCI-N87 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-N87 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
OCI-AML-3	IC₅₀	1.79 μM Compound: MGCD0103	Antiproliferative activity against human OCI-AML-3 cells incubated for 48 hrs Antiproliferative activity against human OCI-AML-3 cells incubated for 48 hrs	[PMID: 36549114]
OCI-AML2	IC₅₀	1.56 μM Compound: MGCD0103	Antiproliferative activity against human OCI-AML2 cells incubated for 48 hrs Antiproliferative activity against human OCI-AML2 cells incubated for 48 hrs	[PMID: 36549114]
PANC-1	IC₅₀	26.774 μM Compound: Mocetinostat	Cytotoxicity against human PANC1 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human PANC1 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
PC-3	IC₅₀	1393 nM Compound: 4; MGCD0103	Antiproliferative activity against human PC-3 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human PC-3 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
PC-9	IC₅₀	345 nM Compound: 4; MGCD0103	Antiproliferative activity against human PC-9 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human PC-9 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
SJSA-1	IC₅₀	3.624 μM Compound: Mocetinostat	Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
SNU-16	IC₅₀	0.142 μM Compound: Mocetinostat	Cytotoxicity against human SNU16 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human SNU16 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
SNU-5	IC₅₀	1.009 μM Compound: Mocetinostat	Cytotoxicity against human SNU5 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human SNU5 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
SW-620	IC₅₀	0.419 μM Compound: Mocetinostat	Cytotoxicity against human SW620 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human SW620 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
Sf9	IC₅₀	102 nM Compound: MGCD0103	Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate	[PMID: 23009203]
Sf9	IC₅₀	> 10000 nM Compound: MGCD0103	Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate	[PMID: 23009203]
T-24	EC₅₀	1.38 μM Compound: 8, MGCD0103	Induction of H3 histone acetylation in human T24 cells relative to MS275 Induction of H3 histone acetylation in human T24 cells relative to MS275	[PMID: 18570366]
T-24	EC₅₀	< 1 μM Compound: A, MGCD0103	Induction of histone H4 hyperacetylation in human T24 cells after 16 hrs by immunoblotting Induction of histone H4 hyperacetylation in human T24 cells after 16 hrs by immunoblotting	[PMID: 19114304]
U-937	IC₅₀	1.37 μM Compound: MGCD0103	Antiproliferative activity against human U-937 cells incubated for 48 hrs Antiproliferative activity against human U-937 cells incubated for 48 hrs	[PMID: 36549114]
ZR-75-1	IC₅₀	1132 nM Compound: 4; MGCD0103	Antiproliferative activity against human ZR-75-1 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ZR-75-1 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]

体外研究
(In Vitro)

Mocetinostat is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC₅₀s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8. Mocetinostat (MGCD0103) exhibits potent and selective antiproliferative activities against a broad spectrum of human cancer cell lines in vitro, and HDAC inhibitory activity is required for these effects. In all cell lines tested, Mocetinostat (MGCD0103) partially inhibits cellular HDAC enzyme activity although the maximal inhibition of activity varies among cell lines from 75% to 85% of total activity. The IC₅₀ of Mocetinostat in intact cancer cells is independent of tissue origin. In A549 cells, MGCD0103 shows dose-dependent inhibition of HDAC activity in whole cells. At high concentrations in A549 cells, Mocetinostat inhibits a maximum of 80% of total activity. In HCT116 cells, Mocetinostat induces a significant S-phase depletion and both G₁ and G₂-M accumulation^[1].

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

体内研究
(In Vivo)

Mocetinostat (MGCD0103) 以剂量依赖性方式显著抑制裸鼠体内人类肿瘤异种移植瘤的生长，其抗肿瘤活性与肿瘤中组蛋白乙酰化的诱导相关^[1]。

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

Clinical Trial

分子量

396.45

Formula

C₂₃H₂₀N₆O

CAS 号

726169-73-9

性状

固体

颜色

White to off-white

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 : 50 mg/mL (126.12 mM; 超声助溶; 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	2.5224 mL	12.6118 mL	25.2236 mL
5 mM	0.5045 mL	2.5224 mL	5.0447 mL
10 mM	0.2522 mL	1.2612 mL	2.5224 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: ≥ 2.08 mg/mL (5.25 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.25 mM); 澄清溶液

此方案可获得 ≥ 2.08 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 20.8 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: 99.68%

选择批次：

Data Sheet (632 KB) SDS (393 KB)

COA (284 KB) LCMS (94 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Fournel M, et al. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther. 2008 Apr;7(4):759-68. [Content Brief]

[2]. Cai J, et al. The Effect of MGCD0103 on CYP450 Isoforms Activity of Rats by Cocktail Method. Biomed Res Int. 2015;2015:517295. [Content Brief]

Cell Assay ^[1]	Cells in 96-well plates are incubated with Mocetinostat at various concentrations for 72 h at 37°C in 5% CO₂. MTT is added at a final concentration of 0.5 mg/mL and incubated with the cells for 4 h before an equal volume of solubilization buffer [50% N,N-dimethylformamide, 20% SDS (pH 4.7)] is added. After overnight incubation, solubilized dye is quantified by reading at 570 nm using a reference at 630 nm. Absorbance values are converted to cell numbers according to a standard growth curve of the relevant cell line. The concentration which reduces cell numbers to 50% relative to DMSO-treated cells is determined as MTT IC₅₀^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]^[2]	Mice^[1] Female CD-1 nude mice, ages 8 to 10 wk are used. Tumor fragments (30 mg), which have been serially passaged thrice in vivo in minimal, are implanted s.c. through a small surgical incision on the flank of the mice while under general anesthesia. Mocetinostat is dissolved in vehicle (PBS acidified with 0.1 N HCl or PEG400/0.2 N HCl saline, 40:60) and dosed p.o. as solutions daily. Tumor volumes and body weight are monitored thrice weekly for at least 2 wk. Each experimental group containe six to eight animals. For pharmacokinetic study, blood is collected from animals at various time points, and plasma samples are analyzed. Rats^[2] Forty rats (220±20 g) are randomly divided into four different dosages of Mocetinostat groups (Low group, Medium group, High group, and control group with 10 rats in each group). Mocetinostat is dissolved in corn oil as suspension at three different concentrations (20, 40, and 80 mg/mL). Three different Mocetinostat groups (Low group, Medium group, and High group) are respectively given Mocetinostat 20, 40, and 80 mg/kg one time by intragastric administration at every morning and last for 7 days. Control group are given saline by same administration method. At 8 days morning, six probe drugs, Bupropion, Phenacetin, Tolbutamide, Metoprolol, Testosterone, and Omeprazole, are mixed in corn oil and given to the rats of three Mocetinostat groups and control group by intragastric administration at a single dosage of 10 mg/kg for Bupropion, Phenacetin, Metoprolol, Testosterone, and Omeprazole and 1 mg/kg for Tolbutamide. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Fournel M, et al. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther. 2008 Apr;7(4):759-68. [Content Brief] [2]. Cai J, et al. The Effect of MGCD0103 on CYP450 Isoforms Activity of Rats by Cocktail Method. Biomed Res Int. 2015;2015:517295. [Content Brief]

Mocetinostat 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	2.5224 mL	12.6118 mL	25.2236 mL	63.0590 mL
	5 mM	0.5045 mL	2.5224 mL	5.0447 mL	12.6118 mL
	10 mM	0.2522 mL	1.2612 mL	2.5224 mL	6.3059 mL
	15 mM	0.1682 mL	0.8408 mL	1.6816 mL	4.2039 mL
	20 mM	0.1261 mL	0.6306 mL	1.2612 mL	3.1530 mL
	25 mM	0.1009 mL	0.5045 mL	1.0089 mL	2.5224 mL
	30 mM	0.0841 mL	0.4204 mL	0.8408 mL	2.1020 mL
	40 mM	0.0631 mL	0.3153 mL	0.6306 mL	1.5765 mL
	50 mM	0.0504 mL	0.2522 mL	0.5045 mL	1.2612 mL
	60 mM	0.0420 mL	0.2102 mL	0.4204 mL	1.0510 mL
	80 mM	0.0315 mL	0.1576 mL	0.3153 mL	0.7882 mL
	100 mM	0.0252 mL	0.1261 mL	0.2522 mL	0.6306 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:

Mocetinostat726169-73-9MGCD0103MGCD 0103MGCD-0103HDACAutophagyApoptosisHistone deacetylasesInhibitorinhibitorinhibit

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Mocetinostat (Synonyms: MGCD0103)

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Mocetinostat (Synonyms: MGCD0103)

Customer Review

Other Forms of Mocetinostat:

Mocetinostat 相关抗体

MCE 顾客使用本产品发表的 21 篇科研文献

Mocetinostat 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 HDAC 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

Mocetinostat 相关抗体:

摩尔计算器

稀释计算器

Mocetinostat 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

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