公告提醒:爱必信所有产品和服务仅用于科学研究,不用于临床应用及其他用途提供产品和服务(也不为任何个人提供产品和服务)! YZ剂描述: 产品名称:PHA-665752 产品别名:PHA 665752; PHA665752 英文别名:PHA 665752;PHA665752 靶点:c-Met ,RON ,Flk1 CAS:477575-56-7 纯度:>98% 外观:light yellow to light brown 保存方法:store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. 描述: PHA-665752是一种有效的,选择性的,ATP竞争性c-MetYZ剂,在无细胞试验中IC50为9 nM,对c-Met的选择性比对 RTKs和 STKs高50倍以上。 溶解性:DMSO : 64.2 mg/mL (100 mM) 体外研究: PHA-665752 significantly inhibits c-Met kinase activity with Ki of 4 nM, and exhibits >50-fold selectivity for c-Met compared with various tyrosine and serine-threonine kinases. PHA-665752 potently inhibits the HGF-stimulated c-Met autophosphorylation with IC50 of 25-50 nM. PHA-665752 also significantly blocks HGF- and c-Met-dependent functions such as cell motility and cell proliferation with IC50 of 40-50 nM and 18-42 nM, respectively. In addition, PHA-665752 potently inhibits HGF-stimulated or constitutive phosphorylation of mediators of downstream of c-Met such as Gab-1, ERK, Akt, STAT3, PLC-γ, and FAK in multiple tumor cell lines. PHA-665752 inhibits cell growth in TPR-MET-transformed BaF3 cells with IC50 of 体内研究:Administration of PHA-665752 induces a dose-dependent tumor growth inhibition of S114 xenografts by 20 %, 39% and 68%, at dose of 7.5, 15, and 30 mg/kg/day, respectively. PHA665752 treatment significantly reduces the tumor growth of NCI-H69, NCI-H441 and A549 in mouse xenografts by 99%, 75%, and 59%, respectively. PHA665752 also significantly inhibits angiogenesis by >85%, due to decreasing the production of vascular endothelial growth factor and increasing the production of the angiogenesis inhibitor thrombospondin-1. 产品信息订购: 产品货号 | 产品名称 | 规格 | 价格 | 大包装及货期 | abs812194 | PHA-665752 | 5mg | 572 | 立即咨询 | 产品更多信息请进入爱必信网站咨询 |