Description
An inhibitor of B-RAF and C-RAF (IC50s = 41, 7, and 2 nM for wild-type B-RAF, B-RAFV600E, and wild-type C-RAF, respectively); cytotoxic to B-RAFV600E-expressing A375 and SK-MEL-28 melanoma cells (IC50s = 57 and 69 nM, respectively), as well as COLO 205 and HCT116 colon and B-CPAP and CAL-62 thyroid cancer cells (IC50s = 116, 65, 43, and 479 nM, respectively); reduces tumor growth in A375, SK-MEL-28, SK-MEL-2, and SK-MEL-30 mouse xenograft models
Formal name: 4-amino-N-[1-[(3-chloro-2-fluorophenyl)amino]-6-methyl-5-isoquinolinyl]-thieno[3,2-d]pyrimidine-7-carboxamide
Synonyms: GDC-5573|HM95573
Molecular weight: 478.9
CAS: 1446113-23-0
Purity: ≥98%
Formulation: A crystalline solid