【产品介绍】：

产品名称 PF-5274857 英文名称 PF-5274857 规格或纯度 98% 英文别名 1-[4-[5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl]piperazin-1-yl]-3-methylsulfonylpropan-1-one；1-[4-(5′-Chloro-3,5-dimethyl-2,4′-bipyridin-2′-yl)piperazin-1-yl] -3- (methylsulfonyl)propan-1-one 运输条件 超低温冰袋运输 生化机理 PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ± 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ± 1.4 nmol/L in cells. This Smo antagonist PF-5274857 showed robust antitumor activity in a mouse model of medulloblastoma with an in vivo IC(50) of 8.9 ± 2.6 nmol/L. PF-5274857 was orally available and metabolically stable in vivo. PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hedgehog (Hh) signaling pathway.PF-5274857 is a hedgehog (Hh) signaling pathway inhibitor acting as a potent and selective Smoothened (Smo) antagonist with an IC50 of 5.8 nM and a Ki of 4.6 nM. PF-5274857 completely blocked downstream gene Gli1 transcriptional activity in Gli-Luc mouse embryonic fibroblast (MEF) cells with an IC50 of 2.7 nM. PF-5274857 is brain penetrant. The compound PF-5274857 showed anti-tumor activity in a mouse medulloblastoma model with an in vivo IC50 of 8.9 nM.CAS编号 1373615-35-0 溶解性 DMSO 93 mg/mL Water 93 mg/mL Ethanol <1 mg/mL 储存温度 -20°C储存 分子量 436.96 分子式 C20H25ClN4O3S PubChem CID 56956240