PHA-665752

• 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
• 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。

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

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

• 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
• InChIKey: OYONTEXKYJZFHA-SSHUPFPWSA-N
• SMILES: Cc1[nH]c(C=C2C(=O)Nc3ccc(S(=O)(=O)Cc4c(Cl)cccc4Cl)cc32)c(C)c1C(=O)N1CCCC1CN1CCCC1
• 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

PHA-665752靶点实验

查看更多实验

实验名称：Cytotoxicity against human CL34 cells expressing MET tyrosine kinase at 200 nM assess... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL993263

实验名称：Cytotoxicity against human KMRC1 cells expressing MET tyrosine kinase at 200 nM asses... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL993266

实验名称：Cytotoxicity against human IGR37 cells expressing MET tyrosine kinase at 200 nM asses... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL993265

实验名称：Cytotoxicity against human NCI-H1993 cells expressing MET tyrosine kinase at 200 nM a... 来源：ChEMBL 靶标：NCI-H1993 External Id：CHEMBL993260

实验名称：Cytotoxicity against human SNU5 cells expressing MET tyrosine kinase at 200 nM assess... 来源：ChEMBL 靶标：SNU-5 External Id：CHEMBL993259

实验名称：Cytotoxicity against human NCI-H2170 cells expressing MET tyrosine kinase at 200 nM a... 来源：ChEMBL 靶标：NCI-H2170 External Id：CHEMBL993262

实验名称：Cytotoxicity against human OE33 cells expressing MET tyrosine kinase at 200 nM assess... 来源：ChEMBL 靶标：OE33 External Id：CHEMBL993261

实验名称：Cytotoxicity against human VMRC-RCZ cells expressing MET tyrosine kinase at 200 nM as... 来源：ChEMBL 靶标：VMRC-RCZ External Id：CHEMBL993272

实验名称：Cytotoxicity against human SW 156 cells expressing MET tyrosine kinase at 200 nM asse... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL993271

实验名称：Cytotoxicity against human MCAS cells expressing MET tyrosine kinase at 200 nM assess... 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL993274

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PHA-665752英文别名

• (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
• 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