化学信息：
| 化学名 | 3-(6-methylpyridin-2-yl)-N-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide |
|
| 简称 | A83-01 | |
| 别名 |
A 83-01, A-83-01, ALK5 Inhibitor IV |
|
| 中文名 | N/A | |
| 化学式 | C25H19N5S | |
| 分子量 | 421.52 | |
| CAS号 | 909910-43-6 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO21mg/ml; Ethanol<1mg/ml |
|
| 溶液配制 | 5mg加入1.19ml DMSO，或者每4.22mg加入1ml DMSO，配制成10mM溶液。SF7917-10mM用DMSO配制。 |
生物信息：
| 产品描述 | A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5nM respectively). | ||||
| 信号通路 | TGF-beta/Smad | ||||
| 靶点 | ALK5 | － | － | － | － |
| IC50 | 12nM | － | － | － | － |
| 体外研究 | A-83-01, an inhibitor of TGF-β type I receptor, increased the expression of Myf5 and MyoD, and enhanced myotube formation. Microarray analysis of HM-1 cells treated with TGF-β1 and/or A-83-01 revealed that A-83-01 efficiently inhibited transcriptional changes that are induced by TGF-β1. -83-01 treatment significantly increased these parameters within 24h that was positively related to pericyte coverage and tumor cell proliferation. Furthermore, apparent diffusion coefficient (ADC) determined by diffusion-weighed imaging was decreased by A-83-01 treatment, suggesting the decrease of tumor interstitial fluid pressure. Vascular function of the tumor improved by A-83-01treatment well assessed on post-Gd-L-enhanced MR images. | ||||
| 体内研究 | The targeting efficacy of single intravenous injections of F-SL combined with A-83-01 was evaluated by measurement of the biodistribution and the antitumor effect in mice bearing murine lung carcinoma M109. A-83-01 temporarily changed the tumor vasculature around 3h post injection. A-83-01 induced 1.7-fold higher drug accumulation of F-SL in the tumor than liposome alone at 24h post injection. | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SF7917-10mM | A83-01 (ALK5抑制剂) | 10mM×0.2ml |
| SF7917-5mg | A83-01 (ALK5抑制剂) | 5mg |
| SF7917-25mg | A83-01 (ALK5抑制剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
