PHA-665752

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Chemical Structure| 477575-56-7 同义名 : -
CAS号 : 477575-56-7
货号 : A717441
分子式 : C32H34Cl2N4O4S
纯度 : 99%+
分子量 : 641.61
MDL号 : MFCD07772270
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(38.96 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 PHA-665752 is an ATP-competitive and selective c-Met inhibitor with Ki value of 4nM, exhibiting >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 dose-dependently inhibited HGF-induced c-Met phosphorylation in A549 cells at concentration ranging in 0.025-0.2μM and suppressed HGF-induced migration in NCI-H441 cells at concentration of 0.1μM. Treatment with 0.1μM PHA-665752 for 3 hours could potently inhibit constitutive signaling through ERK, Akt, FAK, PLC-γ and STAT pathways in GTL-16 cells. Intravenous injection with PHA-665752 could dose-dependently reduce the tumor growth of athymic mice bearing S114 tumors at dose of 7.5, 15 and 30mg/kg, daily for 10 days, and significantly inhibit the tumor growth in the GTL-16 gastric tumor xenograft model, at dose of 25mg/kg, daily for 9 days.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
697 Growth Inhibition Assay IC50=28.7633 μM SANGER
A498 Growth Inhibition Assay IC50=8.28446 μM SANGER
ACN Growth Inhibition Assay IC50=22.2497 μM SANGER
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02002416 - Unknown December 2014 China, Guangdong ... 展开 >> Sun Yat-sen University Cancer Center Guangzhou, Guangdong, China, 510060 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.56mL

0.31mL

0.16mL

7.79mL

1.56mL

0.78mL

15.59mL

3.12mL

1.56mL
参考文献

[1]Ma PC, Schaefer E, et al. A selective small molecule c-MET Inhibitor, PHA665752, cooperates with rapamycin. Clin Cancer Res. 2005 Mar 15;11(6):2312-9.

[2]Christensen JG, Schreck R, 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 Nov 1;63(21):7345-55.