JAB-2485

JAB-2485 is an inhibitor of Aurora A kinase (IC50 = 0. nM). It is selective for Aurora A over Aurora B and Aurora C kinases at 2 µM. JAB-2485 decreases levels of phosphorylated Aurora A kinase in NCI H446 small-cell lung cancer cells (IC50 = 2. nM) and reduces the viability of 11 lung cancer cell lines (IC50s = 29.7-982 nM). JAB-2485 (0. 1, and 3 µM) induces apoptosis and cell cycle arrest at the G2/M phase in NCI H446 cells. It decreases tumor volume without affecting body weight in an NCI H446 mouse xenograft model when administered at doses of 10 or 20 mg/kg per day. InChI: InChI=1S/C25H28ClF2N5O2/c1-14-9-18(29-23(21(14)27)30-20-10-15(2)31-32-20)12-25(24(34)35)7-8-33(16(3)11-25)13-17-5-4-6-19(26)22(17)28/h4-6,9-10,16H,7-8,11-13H2,1-3H3,(H,34,35)(H2,29,30,31,32)/t16-,25-/m1/s1, InChIKey: CEONSWRDFKMFNM-PUAOIOHZSA-N, SMILES: FC(C(Cl)=CC=C1)=C1CN2CC[C@](C(O)=O)(CC3=CC(C)=C(F)C(NC4=CC(C)=NN4)=N3)C[C@H]2C