Imatinib-d3

Imatinib-d3 is intended for use as an internal standard for the quantification of imatinib (Cay-13139) by GC- or LC-MS. 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-d3)-1-piperazinyl]methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide. CAS Number: 1134803-18-1. Synonyms: Genfatinib-d3. Molecular Formula: C29H28D3N7O. Formula Weight: 496.6. Purity: >99% deuterated forms (d1-d3). Formulation: (Request formulation change), A solid. Solubility: DMSO: slightly soluble, Methanol: slightly soluble. SMILES: O=C(NC1=CC=C(C)C(NC2=NC(C3=CC=CN=C3)=CC=N2)=C1)C(C=C4)=CC=C4CN5CCN(C([2H])([2H])[2H])CC5. InChi Code: InChI=1S/C29H31N7O/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/h3-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34)/i2D3. InChi Key: KTUFNOKKBVMGRW-BMSJAHLVSA-N.