NMS-P715

NMS-P715 is an inhibitor of the spindle assembly checkpoint kinase Mps1/TTK (IC50 = 0.182 µM). It is selective for Mps1/TTK over a panel of 59 additional kinases (IC50s = >5 µM for all). NMS-P715 (1 µM) accelerates mitosis, reducing the length of mitosis by approximately 3-fold, in U2OS cells. It induces aneuploidy and apoptosis in A2780 ovarian cancer cells when used at a concentration of 1 µM, as well as inhibits proliferation in a panel of 127 cancer cell lines, including colon, breast, renal, and melanoma cells, with IC50 values ranging from 0.192 to 10 µM. NMS-P715 (90 mg/kg per day) reduces tumor growth in an A2780 mouse xenograft model.Formal Name: N-(2,6-diethylphenyl)-4,5-dihydro-1-methyl-8-[[4-[[(1-methyl-4-piperidinyl)amino]carbonyl]-2-(trifluoromethoxy)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide. CAS Number: 1202055-32-0. Molecular Formula: C35H39F3N8O3. Formula Weight: 676.7. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 304 nm. SMILES: O=C(C1=NN(C)C2=C1CCC3=C2N=C(NC4=CC=C(C(NC5CCN(CC5)C)=O)C=C4OC(F)(F)F)N=C3)NC6=C(CC)C=CC=C6CC. InChi Code: InChI=1S/C35H39F3N8O3/c1-5-20-8-7-9-21(6-2)28(20)42-33(48)30-25-12-10-23-19-39-34(43-29(23)31(25)46(4)44-30)41-26-13-11-22(18-27(26)49-35(36,37)38)32(47)40-24-14-16-45(3)17-15-24/h7-9,11,13,18-19,24H,5-6,10,12,14-17H2,1-4H3,(H,40,47)(H,42,48)(H,39,41,43). InChi Key: JFOAJUGFHDCBJJ-UHFFFAOYSA-N.