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A 77-01
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
A 77-01图片
CAS NO:607737-87-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
25mg电议

产品介绍
A 77-01 是一种转化生长因子 (TGF)-β I 型受体超家族激活素样激酶 ALK5 的有效抑制剂,IC50 为 25 nM。
Cas No.607737-87-1
别名A77-01;A-77-01
化学名4-[5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl]quinoline
Canonical SMILESCC1=CC=CC(=N1)C2=C(C=NN2)C3=CC=NC4=CC=CC=C34
分子式C18H14N4
分子量286.33
溶解度≥ 14.3 mg/mL in DMSO, ≥ 8.84 mg/mL in EtOH with ultrasonic and warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Transforming growth factor (TGF)-β signaling facilitates tumor growth and metastasis in advanced cancer. Use of inhibitors of TGF-β signaling may thus be a novel strategy for the treatment of patients with such cancer. A-77-01 is a close analogue of A-83-01 and has a very similar biological profile of A-83-01. A-83-01 is found to decompose to A-77-01 under certain circumstances and A-77-01 is likely an active component or metabolite of its prodrug A-83-01.
In vitro: A-77-01 and A-83–01 almost completely inhibited the transcriptional activation induced by the constitutively active TGF-β type I receptor (ALK5-TD). A-77-01 and A-83-01 were five to 10 times more potent than the ALK-5 inhibitor SB-431542. In contrast, treatment with 1 μM A-77-01 or 1 μM A-83-01 had no effects on BMP-induced transcriptional activity. However, A-83-01, but not A-77–01, weakly suppressed the transcriptional activity induced by BMP4 at concentrations above 3 μM. A-83-01 and A-77-01 had weak effects on osmotic shock-induced p38 MAPK activity only at high concentrations. A-83-01 and A-77-01 restored the expression of E-cadherin and repressed that of fibronectin and N-cadherin more efficiently than SB-431542 [1].
In vivo: No animal in-vivo data available currently.
Clinical trial: A-77-01 is currently in the preclinical developlent stage and no clinical data are available.
Reference:
[1] Tojo M, Hamashima Y, Hanyu A, Kajimoto T, Saitoh M, Miyazono K, Node M, Imamura T. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005;96(11):791-800.