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抑制剂描述:

产品名称:LY3009120

产品别名:见爱必信官网

英文别名:LY3009120

靶点:Autophagy;Raf

CAS:1454682-72-4

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:

LY3009120 is a potent and selective pan-RAF inhibitor with potential anticancer activity.

溶解性:DMSO :3 mg/mL (7.06 mM)

体外研究:

LY3009120 inhibits the cell growth of A375 and HCT116 cells with the IC50 of 9.2 and 220 μM, respectively. LY3009120 inhibits the tyrosine kinase KDR with the IC50 of 3.9 μM.

体内研究:In rats bearing BRAF V600E ST019VR PDX tumors, LY3009120 (15 or 30 mg/kg, p.o.) shows a dose-dependent tumor growth inhibition. In nude rats bearing A375 xenograft, single dose oral treatment with LY3009120 (3 to 50 mg/kg, p.o.) shows a dose dependent inhibition of phospho-ERK, with a dose for 50% inhibition of phospho-ERK (EC50) of 4.36 mg/kg, with plasma concentration to achieve 50% inhibition of phospho-ERK (EC50) of 68.9 ng/mL or 165 nM.

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