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PHA-665752
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。
PHA-665752图片
CAS NO:477575-56-7
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议
100mg电议

产品介绍
PHA-665752 是一种选择性、ATP 竞争性和活性位点 c-Met 激酶催化活性的抑制剂（Ki=4 nM；IC50=9 nM）。与一组不同的酪氨酸和丝氨酸-苏氨酸激酶相比，PHA-665752 对 c-Met 的选择性 >50 倍。 PHA-665752 诱导细胞凋亡和细胞周期停滞，并表现出细胞减少性抗肿瘤活性。
Cas No.477575-56-7
别名(2R)-1-[[5-[(Z)-[5-[[(2,6-二氯苯基)甲基]磺酰]-1,2-二氢-2-氧代-3H-吲哚-3-亚基]甲基]-2,4-二甲基-1H-吡咯-3-基]羰基]-2-(1-吡咯烷甲基)吡咯烷
化学名(3Z)-5-[(2,6-dichlorophenyl)methylsulfonyl]-3-[[3,5-dimethyl-4-[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]-1H-pyrrol-2-yl]methylidene]-1H-indol-2-one
Canonical SMILESCC1=C(NC(=C1C(=O)N2CCCC2CN3CCCC3)C)C=C4C5=C(C=CC(=C5)S(=O)(=O)CC6=C(C=CC=C6Cl)Cl)NC4=O
分子式C32H34Cl2N4O4S
分子量641.61
溶解度≥ 32.1mg/mL in DMSO
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

PHA-665752 is a potent, ATP-competitive and specific c-Met receptor tyrosine kinase inhibitor with K(i) value of 4 nM and IC50 value of 9nM. PHA-665752 shows more than 50-fold selectivity for c-Met versus other serine-threonine and tyrosine kinases [1].

PHA-665752 has been demonstrated to inhibit hepatocyte growth factor (HGF) and c-Met-mediated cell proliferation, motility, invasion and morphology of pancreatic carcinoma cells BxPC-3, gastric carcinoma cells GTL-16 and lung cancer cells NCI-H441. Additionally, PHA-665752 inhibits the c-MET downstream mediators phosphorylation induced by HGF [1].

In vivo, PHA-665752 inhibits c-Met phosphorylation as well as tumor growth in both S114 and GTL-16 implanted xenograft athymic mice [1].

References:
[1] Christensen JG1, Schreck R, Burrows J, Kuruganti P, Chan E, Le P, Chen J, Wang X, Ruslim L, Blake R, Lipson KE, Ramphal J, Do S, Cui JJ,Cherrington JM, Mendel DB. A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. Cancer Res. 2003 Nov 1;63(21):7345-55.