产品编号 |
产品名称 |
产品包装 |
产品价格 |
SF7917-25mg |
A83-01 (ALK5抑制剂) |
25mg |
1586.00元 |
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
|
参考文献:
1. Furutani Y, Umemoto T, Murakami M. J Cell Biochem. 2011 Feb, 112(2), 614-24.
2. Yamamura S, Matsumura N, Mandai M. Int J Cancer. 2012 Jan 1, 130(1), 20-8.
3. Kawano K, Maitani Y. Yakugaku Zasshi. 2010 Dec, 130(12), 1679-85.
4. Taniguchi Y, Kawano K, Minowa T. Cancer Sci. 2010 Oct, 101(10), 2207-13.
包装清单:
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。
注意事项:
本产品对人体有害,操作时请小心,并注意有效防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放于普通住宅内。
为了您的安全和健康,请穿实验服并戴一次性手套操作。