Masitinib

Masitinib is an inhibitor of the receptor tyrosine kinase c-Kit (IC50 = 200 nM for the recombinant human enzyme). It is also an inhibitor of PDGFRalpha, PDGFRbeta, and Lyn B (IC50s = 540, 800, and 510 nM, respectively). Masitinib inhibits stem cell factor-induced proliferation of Ba/F3 cells expressing wild-type KIT (IC50 = 150 nM), as well as those expressing the KIT mutants KITV559D and KITDelta27 (IC50s = 3 and 5 nM, respectively). It reduces tumor growth in a KITDelta27-expressing Ba/F3 murine model of cancer. Masitinib is also an inhibitor of the severe acute respiratory coronavirus 2 (SARS-CoV-2) main protease (Mpro, Ki = 2.6 µM), also known as 3C-like protease (3CLpro), and inhibits replication of SARS-CoV-2 in infected A549 cells (EC50 = 3.2 µM). It decreases lung and nose viral titers, as well as reduces lung inflammation and increases survival, in ACE2-humanized mice infected with SARS-CoV-2 when administered at a dose of 25 mg/kg.Formal Name: 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]-benzamide. CAS Number: 790299-79-5. Synonyms: AB-1010, Masican, Masiviera. Molecular Formula: C28H30N6OS. Formula Weight: 498.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMSO: 10 mg/ml. lambdamax: 236, 282 nm. SMILES: CC1=C(NC2=NC(C3=CC=CN=C3)=CS2)C=C(NC(C4=CC=C(CN5CCN(C)CC5)C=C4)=O)C=C1. InChi Code: InChI=1S/C28H30N6OS/c1-20-5-10-24(16-25(20)31-28-32-26(19-36-28)23-4-3-11-29-17-23)30-27(35)22-8-6-21(7-9-22)18-34-14-12-33(2)13-15-34/h3-11,16-17,19H,12-15,18H2,1-2H3,(H,30,35)(H,31,32). InChi Key: WJEOLQLKVOPQFV-UHFFFAOYSA-N.