Purity ~98% (HPLC). ATP-competitive inhibitor of Aurora kinases A and B (IC50 values are 0.8 and 5nm for recombinant Aurora B and Aurora A, respectively). Inhibits phosphorylation of Aurora B, histone H3 and Aurora A in cultured MDA-MB-231 cells (IC50 values are ~20, 50 and 150nm respectively). Shown to block cytokinesis; inhibits cellular proliferation in several human tumor cell lines, including HCT-116, HL-60, A549 and H125, and in human xenograft mouse models. Orally available. Sequence: C23H25F3N6O2 Solubility: DMSO (~100mM), Ethanol (~20mM) Molecular Weight: ~474.48
Size
10mg
Concentration
n/a
Applications
n/a
Other Names
PF 03814735 (Aurora Kinases A and B, N-[2-[(1S,4R)-6-[[4-(Cyclobutylamin o)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3, 4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]- acetamide)