PF-5274857

PF-5274857 is a smoothened receptor (Smo) antagonist. It binds to Smo (Ki = 4. nM) and inhibits transcription of Gli1 in mouse embryonic fibroblasts (MEFs, IC50 = 2. nM). In vivo, PF-5274857 inhibits tumor growth and induces tumor regression in a medulloblastoma mouse allograft model when administered at doses less than 10 mg/kg and greater than 10 mg/kg, respectively. InChI: InChI=1S/C20H25ClN4O3S/c1-14-10-15(2)20(23-12-14)16-11-18(22-13-17(16)21)24-5-7-25(8-6-24)19(26)4-9-29(3,27)28/h10-13H,4-9H2,1-3H3 InChIKey: BBVNTTZIOTWDSV-UHFFFAOYSA-N SMILES: CS(=O)(CCC(N1CCN(CC1)C2=NC=C(Cl)C(C3=C(C=C(C=N3)C)C)=C2)=O)=O