PF 03814735

• Supplier: Tocris Bioscience
• Catalog: 1758
• Prices: $245.00, $1,005.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 942487-16-3
• Chemical Name: N-[2-[(1S,4R)-6-[[4-(Cyclobutylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3,4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]-acetamide
• Formula: C23H25F3N6O2
• Molecular Weight: 474.48
• Purity: >98 %
• Description: ATP-competitive inhibitor of Aurora kinases A and B (IC 50 values are 0.8 and 5 nM for recombinant Aurora B and Aurora A, respectively). Inhibits phosphorylation of Aurora B, histone H3 and Aurora A in cultured MDA-MB-231 cells (IC 50 values are approximately 20, 50 and 150 nM 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.

Product References

PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for - PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for

Jani JP, Arcari J, Bernardo V, Bhattacharya SK, Briere D, Cohen BD, Coleman K, Christensen JG, Emerson EO, Jakowski A, Hook K, Los G, Moyer JD, Pruimboom-Brees I, Pustilnik L, Rossi AM, Steyn SJ, Su C, Tsaparikos K, Wishka D, Yoon K, Jakubczak JL. Mol Cancer Ther. 2010 Apr;9(4):883-94.

An integrated genomic approach to identify predictive biomarkers of response to - An integrated genomic approach to identify predictive biomarkers of response to

Hook KE, Garza SJ, Lira ME, Ching KA, Lee NV, Cao J, Yuan J, Ye J, Ozeck M, Shi ST, Zheng X, Rejto PA, Kan JL, Christensen JG, Pavlicek A. Mol Cancer Ther. 2012 Mar;11(3):710-9.

Aurora kinase inhibitors: progress towards the clinic. - Aurora kinase inhibitors: progress towards the clinic.

Kollareddy M, Zheleva D, Dzubak P, Brahmkshatriya PS, Lepsik M, Hajduch M. Invest New Drugs. 2012 Dec;30(6):2411-32.