GW843682X

GW843682X is a reversible, cell-permeable polo-like kinase (PLK) inhibitor. It selectively inhibits Plk1 and Plk3 (IC50s = 2.2 and 9.1 nM, respectively) over PDGFR1beta, VEGFR2, Aurora A, and Cdk2/cyclin A (IC50s = 160, 360, 4,800, and 7,600 nM, respectively), as well as over 30 other kinases, in a cell-free assay. GW843682X also inhibits Plk1 activity in vitro in HeLa cells (IC50 = 0.14 µM in a reporter assay using chimeric Plk1). It inhibits growth in nine cancer cell lines in a panel (IC50s = 0.11-0.7 µM) but not of PC3 human prostate cancer cells (IC50 = 6.82 µM) or non-cancerous human diploid fibroblasts (HDFs, IC50 = 6.14 µM). GW843682X inhibits growth of MES-SA human uterine sarcoma cells, as well as of the drug-resistant, P-glycoprotein-expressing MES-SA/Dx5 subline (IC50s = 0.21 and 0.21 µM, respectively). It also inhibits the growth of patient-derived leukemia cells (IC50s = 2/M cell cycle arrest and apoptosis of H460 human lung and PALL-2 and MOLM13 human leukemia cancer cells in a concentration-dependent manner.Formal Name: 5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide. CAS Number: 660868-91-7. Molecular Formula: C22H18F3N3O4S. Formula Weight: 477.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 40 mg/ml, Ethanol: 4 mg/ml. lambdamax: 296 nm. SMILES: COC1=C(OC)C=C(N=CN2C3=CC(OCC4=CC=CC=C4C(F)(F)F)=C(C(N)=O)S3)C2=C1. InChi Code: InChI=1S/C22H18F3N3O4S/c1-30-16-7-14-15(8-17(16)31-2)28(11-27-14)19-9-18(20(33-19)21(26)29)32-10-12-5-3-4-6-13(12)22(23,24)25/h3-9,11H,10H2,1-2H3,(H2,26,29). InChi Key: JSKUWFIZUALZLX-UHFFFAOYSA-N.