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Biological Activity:
Potent inhibitor of aurora kinases with Ki values to be 0.6, 18 and 4.6 nM for auraro A, B and C isotypes respectively; inhibiting also ABL (Ki=30 nM) and FLT3 (Ki=30 nM) kinases.
References:
EA Harrington et al. VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nature Medicine 10, 262 - 267 (2004) [online]
GM Cheetham et al. Structural basis for potent inhibition of the aurora kinases and a T315I multi-drug resistant mutant form of Abl kinase by VX-680. Cancer Lett. 2007, 251, 323-329.
FJ Giles et al. MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation. Blood 2007, 109, 500-502.
Chemical Name: N-[4-[4-(4-Methylpiperazin-1-yl)-6-(3-methyl-1H-pyrazol-5-ylamino)pyrimidin-2-sulfanyl]phenyl]- cyclopropanecarboxamide
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