ICG1086-PHA-665752
PHA-665752,>99%
【英文同义名】:477575-56-7, PHA 665752, PHA665752, TCMDC-125885
订购信息:(原装进口,常备现货)
品 Pai | 产品名称 | 产品货号 | 规 格 | 目录价(元) |
Gene Operation |
| ICG1086-0005MG | 5 mg | ¥569.00 |
ICG1086-0010MG | 10 mg | ¥959.00 |
ICG1086-0050MG | 50 mg | ¥3,809.00 |
ICG1086-0100MG | 100 mg | ¥6,859.00 |
产品描述 是一种的、ATP竞争性的c-Met小分子YZ剂,其IC50为9 nM。与多种酪氨酸和丝-苏氨酸激酶相比,的选择性要高50多倍。能有效YZHGF刺激的c-Met自磷酸化,以及HGF和c-Met诱导的的表型,如细胞生长(增殖和存活)、细胞运动、侵袭及多种肿瘤细胞形态等 [1]。PHA665752处理能分别降低??NCI-H69(小细胞肺癌)和NCI-H441(非小细胞肺癌)细胞小鼠移植瘤99%和75% [2]。PHA665752能高活性的YZTPR-MET-转化细胞。此c-METYZ剂也可同雷帕霉素合作YZ非小细胞肺癌 [3]。能与Celastrol在体内发挥协同作用,YZc-Met缺陷的肝细胞肿瘤生长 [4]。靶点
靶点 | c-Met |
IC50(半数有效浓度) | 9 nM [1] |
化学特性
储存液配制储存液 (1 ml DMSO体系) | 1 mM | 5 mM | 10 mM | 25 mM |
质量(mg) | 0.6416 | 3.2081 | 6.4161 | 16.0403 |
结构式
使用浓度(仅作参考)的具体使用浓度请参考相关文献,并根据自身实验条件(如实验目的,细胞种类,培养特性等)进行摸索和优化。
参考文献[1] Christensen, J. G. 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 research 63, 7345-7355 (2003).
[2] Puri, N. et al. A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts. Cancer research 67, 3529-3534 (2007).
[3] Ma, P. C., Schaefer, E., Christensen, J. G. & Salgia, R. A selective small molecule c-MET Inhibitor, PHA665752, cooperates with rapamycin. Clinical cancer research : an official journal of the American Association for Cancer Research 11, 2312-2319(2005).
[4] Jiang, H. L. et al. Celastrol exerts synergistic effects with and inhibits tumor growth of c-Met-deficient hepatocellular carcinoma in vivo. Molecular biology reports 40, 4203-4209 (2013).