中文名称: A 83-01 促销
英文名称: A 83-01
CAS No: 909910-43-6
分子式: C25H19N5S
分子量: 421.52
A10095 A 83-01 ≥98% (HPLC) (psaitong)
包装规格:
5mg 25mg 100mg in glass bottle
溶解性:
溶于DMSO(5mg/mL)
产品描述:

基本信息

产品编号:A10095

产品名称:A 83-01

CAS:

909910-43-6

 

储存条件

 

粉末

 

-20℃

四年

分子式:

C25H19N5S

分子量

421.52

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

21mg/mL (49.81mM)

Ethanol

Insoluble

Water

Insoluble

体内(现配现用)

 

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

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。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.3724mL

11.8618mL

23.7237mL

5mM

0.4745mL

2.3724mL

4.7447mL

10mM

0.2372mL

1.1862mL

2.3724mL

 

生物活性

产品描述

一种ALK抑制剂,能抑制TGF-βⅠ型受体ALK-5和活化素IB型受体ALK-4及结节型受体ALK-7诱导的转录活性,其激酶结构域与ALK-5结构域高度相关, IC50分别为 12nM、45nM和7.5nM。

靶点/IC50

ALK5 12nM (IC50)

ALK4 45nM (IC50)

ALK7 7.5nM(IC50)

 

体外研究

A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, reduces the level of ALK-5-induced transcription with an IC50 of 12nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC50s of 45nM and 7.5nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10µM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 µM. A 83- 01 (1-10µM) inhibits TGF-β-induced Smad activation in HaCaT cells[1]. A 83-01 (1µM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation.

体内研究

A 83-01 (50, 150 and 500μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances. A 83-01 (0.5mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells.

 

推荐实验方法(仅供参考)

细胞实验:

 

HM-1 cells are seeded into a 96-well plate and are incubated for 18 hr. A 83-01 (1μM) or vehicle are then added for 12 hr followed by the addition of TGF-β1 (1ng/mL) or vehicle for 60 hr. The number of viable cells in each well is examined using the WST-1 assay.

 

动物实验:

 

Mice
Female B6C3F1 mice used for the in vivo studies are maintained under specific pathogen-free conditions. To evaluate the effect of A 83-01 on the survival of mice bearing peritoneal dissemination, HM-1 cells(1×106 ) are injected into the abdominal cavity via the left flank of the mouse. Starting the next day, A 83-01 (150μg/body) or vehicles (PBS with 0.5% DMSO) are injected into the abdominal cavity three times per week. Mice are euthanized before reaching the moribund state.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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