NMS-1286937

• CAT Number: I000207
• CAS Number: 1034616-18-6
• Molecular Formula: C24H27F3N8O3
• Molecular Weight: 532.52
• Purity: ≥95%
• Target: PLK
• Solubility: DMSO: ≥ 21 mg/mL
• Storage: Store at -20°C
• IC50: 2 nM
• IUPAC Name: 1-(2-hydroxyethyl)-8-[5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)anilino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamide
• InChI: InChI=1S/C24H27F3N8O3/c1-33-6-8-34(9-7-33)15-3-5-18(38-24(25,26)27)17(12-15)30-23-29-13-14-2-4-16-20(22(28)37)32-35(10-11-36)21(16)19(14)31-23/h3,5,12-13,36H,2,4,6-11H2,1H3,(H2,28,37)(H,29,30,31)
• InChIKey: QHLVBNKYJGBCQJ-UHFFFAOYSA-N
• SMILES: CN1CCN(CC1)C2=CC(=C(C=C2)OC(F)(F)F)NC3=NC=C4CCC5=C(C4=N3)N(N=C5C(=O)N)CCO

NMS-1286937（Cat No.:I000207）is a selective and potent inhibitor of Aurora kinase A, a key enzyme involved in regulating cell division by controlling the mitotic spindle formation. By inhibiting Aurora kinase A, NMS-1286937 disrupts proper chromosome alignment and segregation during mitosis, leading to cell cycle arrest and apoptosis in rapidly dividing cancer cells. This compound has shown promise in preclinical studies against various cancers, particularly in tumors with Aurora kinase A overexpression, such as certain types of breast, lung, and ovarian cancers. It is being explored as a targeted therapy in oncology.

Reference

[1]. Beria I, et al. NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett. 2011 May 15;21(10):2969-74.
[2]. Valsasina B, et al. NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies. Mol Cancer Ther. 2012 Apr;11(4):1006-16.
[3]. Casolaro A, et al. The Polo-Like Kinase 1 (PLK1) inhibitor NMS-P937 is effective in a new model of disseminated primary CD56+ acute monoblastic leukaemia. PLoS One. 2013;8(3):e58424.