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)! 抑制剂描述: 产品名称:AZ628 产品别名:见爱必信官网 英文别名:AZ628 靶点:Raf CAS:878739-06-1 纯度:>98% 外观:见爱必信官网 保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. 描述: AZ 628是一种新型pan-Raf抑制剂,作用于BRAF, BRAFV600E和c-Raf-1时,IC50分别为105 nM, 34 nM和29 nM,也抑制VEGFR2, DDR2, Lyn, Flt1, FMS等。AZ628抑制B-Raf,B-RafV600E和c-Raf-1活性,IC50值分别为105,34和29 nM。AZ628也抑制多种酪氨酸蛋白激酶包括VEGFR2, DDR2, Lyn, Flt1, FMS等的激活。 AZ628作用于含B-RafV600E突变的结肠和恶性黑色素瘤细胞系,抑制锚蛋白依赖和非依赖性的生长, 引起细胞周期停滞,且诱导细胞凋亡。 溶解性:DMSO :45.2 mg/mL (100 mM) 体外研究: AZ628 reduces activities of preactivated B-Raf, B-RafV600E, and c-Raf-1 in in vitro kinase assays, with IC50 values of 105, 34 and 29 nM, respectively. AZ628 also inhibits activation of number of tyrosine protein kinases including VEGFR2, DDR2, Lyn, Flt1, FMS and others. AZ628 inhibits anchorage-dependent and -independent growth, causes cell cycle arrest, and induces apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation. AZ-628 suppresses growth in cells expressing K-RASG13D. Inhibition of RAF with AZ-628 suppresses MEK and ERK phosphorylation. AZ-628 selectively affects viability in K-RAS mutant cells. 体内研究: 产品信息订购:
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