Belvarafenib

Belvarafenib is 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). It is 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). Belvarafenib 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. CAS Number: 1446113-23-0. Synonyms: GDC-5573, HM95573. Molecular Formula: C23H16ClFN6OS. Formula Weight: 478.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml. lambdamax: 215, 316 nm. SMILES: O=C(C1=CSC2=C1N=CN=C2N)NC3=C(C)C=CC4=C3C=CN=C4NC5=CC=CC(Cl)=C5F. InChi Code: InChI=1S/C23H16ClFN6OS/c1-11-5-6-13-12(7-8-27-22(13)30-16-4-2-3-15(24)17(16)25)18(11)31-23(32)14-9-33-20-19(14)28-10-29-21(20)26/h2-10H,1H3,(H,27,30)(H,31,32)(H2,26,28,29). InChi Key: KVCQTKNUUQOELD-UHFFFAOYSA-N.