PHA-665752

更新时间：2024-01-08 11:17:33

PHA-665752结构式	常用名	PHA-665752	英文名	PHA-665752
	CAS号	477575-56-7	分子量	641.608
	密度	1.4±0.1 g/cm3	沸点	890.2±65.0 °C at 760 mmHg
	分子式	C₃₂H₃₄Cl₂N₄O₄S	熔点	N/A
	MSDS	中文版美版	闪点	492.2±34.3 °C

PHA-665752用途

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。

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
英文别名	更多

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.

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.

密度	1.4±0.1 g/cm3
沸点	890.2±65.0 °C at 760 mmHg
分子式	C₃₂H₃₄Cl₂N₄O₄S
分子量	641.608
闪点	492.2±34.3 °C
精确质量	640.167786
PSA	110.96000
LogP	4.00
外观性状	light yellow to light brown
蒸汽压	0.0±0.3 mmHg at 25°C
折射率	1.656
储存条件	Store at +4°C
水溶解性	DMSO: ≥20mg/mL

5-[5-(2,6-dichl...

477574-82-6

(R)-(-)-1-(2-吡咯...

60419-23-0

PHA-665752

477575-56-7

文献：US2003/125370 A1, ;

PHA-665752上游产品 1
CAS号60419-23-0 (R)-(-)-1-(2-吡咯...
PHA-665752下游产品 0

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