Sonic hedgehog (Shh) signaling is initiated by binding of the ligand, Shh, to the receptor Patched 1, which relieves suppression by the associated receptor Smoothened (Smo). PF-05274857 is an antagonist which binds Smo (Ki = 4.6 nM), blocking Gli1 transcription in cells stimulated with Shh (IC50 = 2.7 nM). When administered orally, it distributes through plasma to skin and tumor and remains metabolically stable. PF-05274857 also penetrates the blood-brain barrier and inhibits Smo activity in the brain.

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

Soluble in DMSO

1.Rohner, A.,Spilker, M.E.,Lam, J.L., et al. Effective targeting of hedgehog signaling in a medulloblastoma model with PF-5274857, a potent and selective smoothened antagonist that penetrates the blood-brain barrier. Molecular Cancer Therapeutics 11(1), 57-65 (2012).