MLN0905

MLN0905 is an inhibitor of polo-like kinase 1 (Plk1, IC50 = 2 nM). It inhibits 95% of Plk1 activity but also inhibits the activity of 10 additional kinases by greater than or equal to 90% in a panel of 359 kinases at 1 µM. MLN0905 reduces phosphorylation of histone H3 at serine 10 (H3S10Ph), a marker of cell cycle arrest at prometaphase, in HT-29 colorectal cancer cells (EC30 = 9 nM). It inhibits proliferation in a panel of six human lymphoma cell lines with IC50 values ranging from 3.2 to 24 nM. MLN0905, alone or in combination with rituximab, increases survival in an OCI LY-19 metastatic lymphoma mouse xenograft model.Formal Name: 2-[[5-[3-(dimethylamino)propyl]-2-methyl-3-pyridinyl]amino]-5,7-dihydro-9-(trifluoromethyl)-6H-pyrimido[5,4-d][1]benzazepine-6-thione. CAS Number: 1228960-69-7. Molecular Formula: C24H25F3N6S. Formula Weight: 486.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. SMILES: FC(F)(F)C1=CC=C2C(NC(CC3=CN=C(NC4=C(C)N=CC(CCCN(C)C)=C4)N=C32)=S)=C1. InChi Code: InChI=1S/C24H25F3N6S/c1-14-19(9-15(12-28-14)5-4-8-33(2)3)31-23-29-13-16-10-21(34)30-20-11-17(24(25,26)27)6-7-18(20)22(16)32-23/h6-7,9,11-13H,4-5,8,10H2,1-3H3,(H,30,34)(H,29,31,32). InChi Key: CODBZFJPKJDNDT-UHFFFAOYSA-N.