Pf 5274857 Hydrochloride, High Affinity And Selective Smoothened (Smo) Receptor Antagonist, Each

Details:

Pf 5274857 hydrochloride is a high affinity and selective smoothened (smo) receptor antagonist (ki = 4.6 Nm). Exhibits >1000-fold selectivity for smo over a panel of other receptors, ion channels and enzymes. Inhibits shh-induced hedgehog signaling in mef cells. Induces tumor regression in a medulloblastoma allograft mouse model. Orally available and brain penetrant.