Glasdegib (PF-04449913)

Description: Glasdegib (formerly known as PF-04449913; PF4449913; PF04449913; PF-4449913) is a novel, potent, and orally bioavailable small-molecule inhibitor of Smoothened (Smo) in the Hedgehog (Hh) signaling pathway with potential antitumor activity. It inhibits Smoothened (Smo) with an IC50 of 5 nM. The Hh signaling pathway plays an important role in cellular growth, differentiation and repair. Constitutive activation of Hh pathway signaling has been observed in various types of cancers. Glasdegib significantly reduces medulloblastoma growth in a Ptch1+/-p53+/- allograft model at doses that decreased murine Shh target gene expression. In stromal co-culture experiments, FACS analysis demonstrates a significant reduction in BC LSC by PF-04449913 when compared with normal progenitors.

References: ACS Med Chem Lett. 2011 Dec 21; 3(2):106-11.

Related CAS#: 2030410-25-2 (Maleate); 1095173-27-5 (free base); 1095173-64-0 (HCl); 1352568-48-9 (2HCl)