PHA-665752

P H A - 6 6 5 7 5 2

更新时间：2024-04-20 02:00:57

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PHA-665752 名称

中文名

(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
英文名

PHA-665752 hydrate
中文别名
英文别名

2H-Indol-2-one, 5-[[(2,6-dichlorophenyl)methyl]sulfonyl]-3-[[3,5-dimethyl-4-[[(2R)-2-(1-pyrrolidinylmethyl)-1-pyrrolidinyl]carbonyl]-1H-pyrrol-2-yl]methylene]-1,3-dihydro-, (3Z)- |(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 |TCMDC-125885 |(3Z)-5-[(2,6-Dichlorobenzyl)sulfonyl]-3-[(3,5-dimethyl-4-{[(2R)-2-(1-pyrrolidinylmethyl)-1-pyrrolidinyl]carbonyl}-1H-pyrrol-2-yl)methylene]-1,3-dihydro-2H-indol-2-one |(3Z)-5-[(2,6-Dichlorobenzyl)sulfonyl]-3-[(3,5-dimethyl-4-{[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]carbonyl}-1H-pyrrol-2-yl)methylene]-1,3-dihydro-2H-indol-2-one |PHA-665752 |

PHA-665752 生物活性

描述

PHA-665752是ATP竞争性c-Met选择性抑制剂，IC50为9 nM，比对RTKs和STKs的抑制性高50倍。
相关类别

信号通路 >> 自噬 >> 自噬信号通路 >> 蛋白酪氨酸激酶 >> c-Met的/HGFR 研究领域 >> 癌症
参考文献

[1]. Christensen JG, et al. 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, 63(21), 7345-7355. [2]. Ma PC, et al. A selective small molecule c-MET Inhibitor, PHA665752, cooperates with rapamycin. Clin Cancer Res, 2005, 11(6), 2312-2319. [3]. Puri N, et al. A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts. Cancer Res, 2007, 67(8), 3529-3534. [4]. Tsubaki M, et al. Contributions of MET activation to BCR-ABL1 tyrosine kinase inhibitor resistance in chronic myeloid leukemia cells. Oncotarget. 2017 Jun 13;8(24):38717-38730.

PHA-665752 物理化学性质

PHA-665752 合成路线

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