Description
A Smoothened receptor antagonist; binds to human recombinant Smo expressed in HEK293T cells (IC50 = 1.1 µM); inhibits Gli1-mediated hedgehog signaling in a reporter assay (IC50 = 1.5 µM); an inhibitor of 11β-hydroxy steroid dehydrogenase-1; reduces tumor growth in a murine medulloblastoma mouse allograft model at 40 and 80 mg/kg per day); induces tumor regression at 80 mg/kg twice per day; reduces expression of the hedgehog pathway-associated transcription factor Gli1 in tumor tissue
Formal name: 5-(3,3-difluorocyclobutyl)-3-[4-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]bicyclo[2.2.2]oct-1-yl]-1,2,4-oxadiazole
Synonyms:
Molecular weight: 493.5
CAS: 935273-79-3
Purity: ≥98%
Formulation: A crystalline solid