MK-0457

The Aurora kinases (A, B, and C) are a family of serine-threonine kinases that regulate various stages of mitotic function. With significant roles in cell cycle and cell division, Aurora kinase gene amplification and overexpression are linked to tumorigenesis. MK-0457 is a potent pan-Aurora kinase inhibitor but favors Aurora A (Ki = 0.6 nM) over Aurora B (Ki = 18 nM) or Aurora C (Ki = 4.6 nM). It shows selectivity against a panel of more than 190 different protein kinases. MK-0457 effectively inhibits proliferation of several different cell lines of clear cell renal carcinoma (IC50s = 2/M phase.Formal Name: N-[4-[[4-(4-methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]-cyclopropanecarboxamide. CAS Number: 639089-54-6. Synonyms: Tozasertib, VX-680. Molecular Formula: C23H28N8OS. Formula Weight: 464.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7) (1:10): 0.1 mg/ml, DMSO: 15 mg/ml. lambdamax: 253 nm. SMILES: CN1CCN(C2=CC(NC3=NNC(C)=C3)=NC(SC4=CC=C(NC(C5CC5)=O)C=C4)=N2)CC1. InChi Code: InChI=1S/C23H28N8OS/c1-15-13-20(29-28-15)25-19-14-21(31-11-9-30(2)10-12-31)27-23(26-19)33-18-7-5-17(6-8-18)24-22(32)16-3-4-16/h5-8,13-14,16H,3-4,9-12H2,1-2H3,(H,24,32)(H2,25,26,27,28,29). InChi Key: GCIKSSRWRFVXBI-UHFFFAOYSA-N.