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PHA-665752
c-Met的ATP竞争性、有效的、选择性抑制剂

PHA-665752

产品编号:A2307
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规格 单价 库存 订购数量
10mM (in 1mL DMSO) ¥900.00 现货
10mg ¥800.00 现货
50mg ¥3,300.00 现货
100mg ¥5,700.00 现货

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Sample solution is provided at 25 µL, 10mM.

引用文献

1. Xia Y, Xia YF, et al. "Madecassoside ameliorates bleomycin-induced pulmonary fibrosis in mice through promoting the generation of hepatocyte growth factor via PPAR-γ in colon. Br J Pharmacol." 2016 Apr;173(7):1219-35.  PMID:26750154

质量控制

质量控制和MSDS

批次:

化学结构

PHA-665752

相关生物数据

PHA-665752

相关生物数据

PHA-665752

相关生物数据

PHA-665752

PHA-665752 Dilution Calculator

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PHA-665752 Molarity Calculator

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化学性质

CAS号 477575-56-7 SDF Download SDF
化学名 (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
SMILES CC1=C(NC(=C1C(=O)N2CCCC2CN3CCCC3)C)C=C4C5=C(C=CC(=C5)S(=O)(=O)CC6=C(C=CC=C6Cl)Cl)NC4=O
分子式 C32H34Cl2N4O4S 分子量 641.61
溶解度 ≥32.1mg/mL in DMSO 储存条件 Store at -20°C
物理性状 A solid 运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

描述 PHA-665752是c-Met的ATP竞争性、有效的、选择性抑制剂(IC50值9 nM),对c-Met的选择性是RTKs或STKs的50多倍。
靶点 c-Met          
IC50 9 nM          

View Related Products By Research Topics

研究更新

1. Celastrol exerts synergistic effects with PHA-665752 and inhibits tumor growth of c-Met-deficient hepatocellular carcinoma in vivo. Mol Biol Rep. 2013 Jul;40(7):4203-9. doi: 10.1007/s11033-013-2501-y. Epub 2013 May 7.
Abstract
PHA665752 is a c-Met inhibitor that exhibits anti-tumor activity only in c-Met-positive tumor cells. The combination of PHA6657552 and Celastrol is a potential therapy of c-Met-deficient tumors for their demonstrated antitumor effects in c-Met-deficient hepatocellular carcinoma cells and xenografts.
2. A selective small molecule inhibitor of c-Met, PHA-665752, reverses lung premalignancy induced by mutant K-ras. Mol Cancer Ther. 2008 Apr;7(4):952-60. doi: 10.1158/1535-7163.MCT-07-2045.
Abstract
PHA-665752, a c-Met inhibitor, inhibited lung tumorigenesis in Kras(LA1) mice and induced apoptosis in LKR-13 cells and MECs, where apoptosis in MECs was induced by c-Met inhibition.
3. Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752. Proc Natl Acad Sci U S A. 2006 Feb 14;103(7):2316-21. Epub 2006 Feb 6.
Abstract
Gastric cancer cells with high levels of MET are extraordinarily susceptible to PHA-665752, which induces massive apoptosis.

产品描述

PHA-665752是ATP竞争性、有效的、特定的c-Met受体酪氨酸激酶抑制剂,Ki值4 nM,IC50值9 nM。PHA-665752对c-Met的选择性是丝氨酸/苏氨酸激酶和酪氨酸激酶的50多倍[1]。

已证实PHA-665752能抑制肝细胞生长因子(HGF)和c-Met调节的胰脏癌细胞BxPC-3、胃癌细胞GTL-16和肺癌细胞NCI-H441的细胞增殖、运动性、入侵和形态学。此外,PHA-665752抑制HGF引起的c-Met下游介质的磷酸化[1]。

在体内,PHA-665752在移植了无胸腺的小鼠S114和GTL-16中抑制c-Met磷酸化及肿瘤生长[1]。

参考文献:
[1]. Christensen JG1, Schreck R, Burrows J, Kuruganti P, Chan E, Le P, Chen J, Wang X, Ruslim L, Blake R, Lipson KE, Ramphal J, Do S, Cui JJ,Cherrington JM, Mendel DB. 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.