CX-6258

The family of Pim (Provirus Integration site for Moloney murine leukemia virus) proteins are serine/threonine kinases involved in cell survival and cell proliferation. CX-6258 is a potent, reversible inhibitor of Pim-1, -2, and -3 (IC50s = 5, 25, and 16 nM, respectively). It demonstrates excellent selectivity, inhibiting only FLT3 from a panel of 107 additional kinases. CX-6258 dose-dependently blocks the phosphorylation of the Pim targets Bad, 4E-BP1, and NKX3.1. It acts synergistically with the chemotherapeutics doxorubicin and paclitaxel, presumably because CX-6258 impairs Pim-mediated enhanced expression of P-glycoprotein. CX-6258 is orally bioavailable and inhibits the growth of MV4-11 xenografts in mice.Formal Name: (3E)-5-chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-2H-indol-2-one. CAS Number: 1202916-90-2. Synonyms: Pim-Kinase Inhibitor X. Molecular Formula: C26H24ClN3O3. Formula Weight: 461.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 5 mg/ml. lambdamax: 212, 258, 403 nm. SMILES: O=C(N1CCCN(C)CC1)C2=CC=CC(C3=CC=C(/C=C4C(NC5=C/4C=C(Cl)C=C5)=O)O3)=C2. InChi Code: InChI=1S/C26H24ClN3O3/c1-29-10-3-11-30(13-12-29)26(32)18-5-2-4-17(14-18)24-9-7-20(33-24)16-22-21-15-19(27)6-8-23(21)28-25(22)31/h2,4-9,14-16H,3,10-13H2,1H3,(H,28,31)/b22-16+. InChi Key: KGBPLKOPSFDBOX-CJLVFECKSA-N.