PF-5274857 freebase 是有效的、具有口服活性的、选择性的、可透过血脑屏障的Smo拮抗剂，其IC50=5.8 nM，Ki=4.6 nM。它有用于包括激活的 Hh 途径驱动的脑肿瘤和脑转移在内的多种肿瘤的研究潜力。

PF-5274857 is an effective and selective hedgehog signaling pathway inhibitor (IC50: 5.8 nM and a Ki: 4.6 nM). PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.PF-5274857 was found to effectively penetrate the blood-brain barrier and inhibit Smo activity in the brain of primary medulloblastoma mice, resulting in improved animal survival rates. PF-5274857 was orally available and metabolically stable in vivo.

1373615-35-0

C20H25ClN4O3S

436.96

PF-5274857 freebase

DMSO:125 mg/mL (286.07 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years