Imatinib (mesylate)

Imatinib is an inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit. It inhibits ligand-stimulated autophosphorylation of PDGFR and c-Kit (IC50s = ~0.3 and ~0.1 µM, respectively). Imatinib inhibits the proliferation of Bcr-Abl-dependent R10(-) cells (IC50s = ~35-40 nM) and HMC-1 cells expressing constitutively active c-Kit in a concentration-dependent manner.{47196, 20180} It prolongs survival in a mouse model of chronic myeloid leukemia when administered at a dose of 100 mg/kg twice per day. Imatinib (25 and 50 µM) also inhibits the replication of Middle East respiratory syndrome coronavirus (MERS-CoV) and severe acute respiratory syndrome CoV (SARS-CoV) in Vero E6 cells. It reduces viral titers in Vero cells infected with infectious bronchitis virus (IBV), a coronavirus, when used at a concentration of 10 µM via inhibition of IBV surface glycoprotein protein-induced syncytia formation and virus-cell fusion. Formulations containing imatinib have been used in the treatment of various cancers.Formal Name: 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide, monomethanesulfonate. CAS Number: 220127-57-1. Synonyms: CGP57148B, STI-571. Molecular Formula: C29H31N7O . CH4SO3. Formula Weight: 589.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 14 mg/ml, Ethanol: 0.2 mg/ml, PBS (pH 7.2): 2 mg/ml. lambdamax: 238, 271 nm. SMILES: CN1CCN(CC1)Cc1ccc(cc1)C(=O)Nc1ccc(C)c(c1)Nc1nccc(n1)c1cccnc1CS(=O)(=O)O. InChi Code: InChI=1S/C29H31N7O.CH4O3S/c1-21-5-10-25(18-27(21)34-29-31-13-11-26(33-29)24-4-3-12-30-19-24)32-28(37)23-8-6-22(7-9-23)20-36-16-14-35(2)15-17-36,1-5(2,3)4/h3-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34),1H3,(H,2,3,4). InChi Key: YLMAHDNUQAMNNX-UHFFFAOYSA-N.