477575-56-7

• 常用中文名：PHA-665752
• 常用英文名：PHA-665752
• CAS号：477575-56-7
• 分子式：C₃₂H₃₄Cl₂N₄O₄S
• 分子量：641.608
• 相关类别： 生物化工 抑制剂 蛋白酪氨酸激酶
• 发布时间：2018-12-31 18:15:02
• 更新时间：2026-07-11 13:37:47
• 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。

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: PHA-665752,ATP竞争性C-MET抑制剂; (R,Z)-5-((2,6-二氯苄基)磺酰基)-3-((3,5-二甲基-4-(2-(吡咯烷-1-基甲基)吡咯烷-1-羰基)-1H-吡咯-2-基)亚甲基)二氢吲哚-2-酮; PHA-665752 抑制剂; PHA-665752水合物; PHA-665752 10mM * 1mL in DMSO试剂; C-MET抑制剂(PHA-665752); PHA-665752 5mg试剂
• 英文别名: PHA 665752 (2R)-1-[[5-[(Z)-[5-[[(2,6-Dichlorophenyl)methyl]sulfonyl]-1,2-dihydro-2-oxo-3H-indol-3-ylidene]methyl]-2,4-dimethyl-1H-pyrrol-3-yl]carbonyl]-2-(1-pyrrolidinylmethyl)pyrrolidine; (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; (R,Z)-5-(2,6-dichlorobenzylsulfonyl)-3-((3,5-dimethyl-4-(2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl)-1H-pyrrol-2-yl)methylene)indolin-2-one; PHA-665752/PHA665752; (2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]carbonyl]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE PHA; (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, 10 mM in DMSO; (R,Z)-5-((2,6-Dichlorobenzyl)sulfonyl)-3-((3,5-dimethyl-4-(2-(pyrrolidin-1-ylmethyl)pyrrolidin; 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); 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; (2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]carbonyl]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE; PHA-665752 c-Met Inhibitor; (2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]carbonyl]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE //BP

物化性质

• 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

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.

合成路线

477574-82-6 60419-23-0 ~% 477575-56-7

文献：US2003/125370 A1, ;

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