2. Protein Tyrosine Kinase/RTK Epigenetics Stem Cell/Wnt JAK/STAT Signaling Apoptosis
  3. Bcr-Abl PDGFR c-Kit Src JAK Apoptosis
  4. HG-7-85-01

HG-7-85-01 是一种 Bcr-Abl，PDGFRα，Kit 和 Src 激酶的野生型和看门突变形式的 II 型 ATP 竞争性抑制剂。HG-7-85-01 抑制 T315I 突变型 Bcr-Abl (T315I mutant Bcr-Abl) 激酶，KDR 和 RET，IC50 为 3 nM，20 nM 和 30 nM，对其他激酶的抑制作用很小或没有抑制作用 (IC50>2 μM)。HG-7-85-01 通过诱导细胞凋亡 (apoptosis) 和抑制细胞周期进程来抑制细胞增殖。

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

HG-7-85-01 Chemical Structure

HG-7-85-01 Chemical Structure

CAS No. : 1258391-13-7

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 数量
5 mg ￥2050
In-stock
10 mg ￥3250
In-stock
25 mg ￥6500
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

HG-7-85-01 相关抗体

Top Publications Citing Use of Products

查看 PDGFR 亚型特异性产品:

查看所有亚型
PDGFR PDGFRβ PDGFRα

查看 Src 亚型特异性产品:

查看所有亚型
Lck

查看 JAK 亚型特异性产品:

查看所有亚型
JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression[1].

IC50 & Target

Bcr-AblT315I

3 nM (IC50)

PDGFRα

440 nM (IC50)

JAK1

120 nM (IC50)

KDR

20 nM (IC50)

RET

30 nM (IC50)

MK5

560 nM (IC50)

体外研究
(In Vitro)

HG-7-85-01 (0-1 μM; 24 hours; BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells) treatment leads to G0G1 arrest of BCR-ABL-expressing cells[1].
HG-7-85-01 (0-1 μM; 72 hours; BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells) treatment also leads to induction of apoptosis of BCR-ABL-expressing cells[1].
HG-7-85-01 treatment potently and selectively inhibits the proliferation of 32D- and Ba/F3 cells expressing nonmutant BCR-ABL and the BCR-ABL-T315I gatekeeper mutant. HG-7-85-01 shows higher potency against nonmutant BCR-ABL and BCR-ABL-T315I (IC50 = 0.06-0.14 μM)[1].
HG-7-85-01 inhibits BCR-ABL kinase activity in a concentration-dependent manner, suggesting selective targeting of the BCR-ABL kinase as the mechanism of action of HG-7-85-01[1].
HG-7-85-01 potently inhibits the proliferation of Ba/F3 cells expressing the Kit-T670I gatekeeper mutation (Ba/F3- Kit-T670I) and Ba/F3 cells expressing TEL/PDGFRβ and no effect on parental Ba/F3 cells. HG-7-85-01 inhibits Kit, PDGFR phosphorylation in a concentration-dependent manner[1].
The PDGFRα-T674M and PDGFRα-T674I gatekeeper mutant variants are highly responsive to HG-7-85-01 and significant IL-3 rescue[1].
HG-7-85-01 inhibits the proliferation of Ba/F3 cells transformed with human c-Src (EC50 = 190 nM), T338I Src (EC50 = 290 nM), and T338M Src (EC50 = 150 nM; chicken c-Src numbering). And potently inhibits the proliferation of exon 11 Kit mutant-expressing cells, exon 9 kit mutant-expressing cells are significantly less responsive[1].

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

HG-7-85-01 相关抗体:

Cell Cycle Analysis[1]

Cell Line: BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells
Concentration: 0 μM, 0.01 μM, 0.1 μM and 1 μM
Incubation Time: 24 hours
Result: Led to G0G1 arrest of BCR-ABL-expressing cells.

Apoptosis Analysis[1]

Cell Line: BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells
Concentration: 0 μM, 0.01 μM, 0.1 μM and 1 μM
Incubation Time: 72 hours
Result: Led to induction of apoptosis of BCR-ABL-expressing cells.
体内研究
(In Vivo)

HG-7-85-01 has limited oral bioavailability (BAV % F mouse = 5 %, rat = 19 %), a moderate half life (T1/2 mouse =1.1 h rat = 5.8 hours), a relative low maximal serum concentration (Cmax mouse = 106 ng/mL at 10 mg/kg , rat = 292 ng/mL and 2 mg/kg ) and a relatively high clearance (Cl mouse = 23 ml/min/kg, rat = 13 ml/min/kg) [1].

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

608.68

Formula

C31H31F3N6O2S
CAS 号
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (205.36 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 1.6429 mL 8.2145 mL 16.4290 mL
5 mM 0.3286 mL 1.6429 mL 3.2858 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

g

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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

HG-7-85-01 相关分类

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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6429 mL 8.2145 mL 16.4290 mL 41.0725 mL
5 mM 0.3286 mL 1.6429 mL 3.2858 mL 8.2145 mL
10 mM 0.1643 mL 0.8214 mL 1.6429 mL 4.1072 mL
15 mM 0.1095 mL 0.5476 mL 1.0953 mL 2.7382 mL
20 mM 0.0821 mL 0.4107 mL 0.8214 mL 2.0536 mL
25 mM 0.0657 mL 0.3286 mL 0.6572 mL 1.6429 mL
30 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3691 mL
40 mM 0.0411 mL 0.2054 mL 0.4107 mL 1.0268 mL
50 mM 0.0329 mL 0.1643 mL 0.3286 mL 0.8214 mL
60 mM 0.0274 mL 0.1369 mL 0.2738 mL 0.6845 mL
80 mM 0.0205 mL 0.1027 mL 0.2054 mL 0.5134 mL
100 mM 0.0164 mL 0.0821 mL 0.1643 mL 0.4107 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:

HG-7-85-011258391-13-7Bcr-AblPDGFRc-KitSrcJAKApoptosisPlatelet-derived growth factor receptorSCFRCD117Janus kinaseATPBCR-ABLPDGFRαKDRRETDDR1tyrosinekinasescell-cycleInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   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：

Bulk Inquiry

Inquiry Information

产品名称：
HG-7-85-01
目录号：
HY-15814
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   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：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z