BLU-285

BLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor alpha (PDGFRalpha) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRalphaD842V, respectively). It is >150-fold selective for KITD816V and PDGFRalphaD842V over a kinase panel at a concentration of 3 µM. BLU-285 also has activity against a panel of KIT and PDGFRalpha loop mutants identified in patients with gastrointestinal stromal tumors (GISTs, IC50s = D814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRalpha-driven malignancies.Formal Name: (alphaS)-(4-fluorophenyl)-alpha-methyl-2-[4-[6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]-1-piperazinyl]-5-pyrimidinemethanamine. CAS Number: 1703793-34-3. Synonyms: Avapritinib. Molecular Formula: C26H27FN10. Formula Weight: 498.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 66 mg/ml, Ethanol: 3 mg/ml. lambdamax: 254, 309 nm. SMILES: C[C@@](C1=CC=C(F)C=C1)(N)C(C=N2)=CN=C2N3CCN(C4=NC=NN5C4=CC(C6=CN(C)N=C6)=C5)CC3. InChi Code: InChI=1S/C26H27FN10/c1-26(28,20-3-5-22(27)6-4-20)21-13-29-25(30-14-21)36-9-7-35(8-10-36)24-23-11-18(16-37(23)33-17-31-24)19-12-32-34(2)15-19/h3-6,11-17H,7-10,28H2,1-2H3/t26-/m0/s1. InChi Key: DWYRIWUZIJHQKQ-SANMLTNESA-N.