详情描述
PF-5274857 is a potent, orally active and selective hedgehog (Hh) signaling pathway inhibitor with an IC50 of 5.8 nM and a Ki of 4.6 nM. 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. 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.
Product information
CAS Number: 1373615-35-0
Molecular Weight: 436.96
Formula: C20H25ClN4O3S
Chemical Name: 1-(4-{5'-chloro-3,5-dimethyl-[2,4'-bipyridin]-2'-yl}piperazin-1-yl)-3-methanesulfonylpropan-1-one
Smiles: CS(=O)(=O)CCC(=O)N1CCN(CC1)C1=CC(=C(Cl)C=N1)C1=NC=C(C)C=C1C
InChiKey: BBVNTTZIOTWDSV-UHFFFAOYSA-N
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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.