PF-03814735

• CAT Number: I005603
• CAS Number: 942487-16-3
• Molecular Formula: C₂₃H₂₅F₃N₆O₂
• Molecular Weight: 474.48
• Purity: ≥95%
• Target: Aurora Kinase
• Solubility: DMSO: ≥ 47 mg/mL
• Storage: -20°C
• IC50: 0.8 nM(Aurora A); 5 nM(Aurora B); 10 nM(Flt1); 22 nM(FAK); 30 nM(TrkA)
• IUPAC Name: N-[2-[(1R,8S)-4-[[4-(cyclobutylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-11-azatricyclo[6.2.1.02,7]undeca-2(7),3,5-trien-11-yl]-2-oxoethyl]acetamide
• InChI: InChI=1S/C23H25F3N6O2/c1-12(33)27-11-20(34)32-18-7-8-19(32)16-9-14(5-6-15(16)18)30-22-28-10-17(23(24,25)26)21(31-22)29-13-3-2-4-13/h5-6,9-10,13,18-19H,2-4,7-8,11H2,1H3,(H,27,33)(H2,28,29,30,31)/t18-,19+/m0/s1
• InChIKey: RYYNGWLOYLRZLK-RBUKOAKNSA-N
• SMILES: CC(=O)NCC(=O)N1C2CCC1C3=C2C=CC(=C3)NC4=NC=C(C(=N4)NC5CCC5)C(F)(F)F

PF-03814735（Cat No.:I005603） is a highly potent inhibitor of Aurora kinases A and B, which are key regulators of cell division. It acts by competitively binding to the ATP-binding site of these kinases, thereby disrupting their activity. With IC50 values of 0.8 nM for Aurora A and 5 nM for Aurora B, PF-03814735 shows strong inhibitory effects on both isoforms. It’s oral availability and reversible binding make it a promising candidate for the development of anticancer therapies targeting aberrant cell division.

Reference

1:An integrated genomic approach to identify predictive biomarkers of response to the aurora kinase inhibitor PF-03814735. 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. doi: 10.1158/1535-7163.MCT-11-0184. Epub 2012 Jan 5. PMID: 22222631 Free Article2:Phase I, open-label, multicentre, dose-escalation, pharmacokinetic and pharmacodynamic trial of the oral aurora kinase inhibitor PF-03814735 in advanced solid tumours. Schöffski P, Jones SF, Dumez H, Infante JR, Van Mieghem E, Fowst C, Gerletti P, Xu H, Jakubczak JL, English PA, Pierce KJ, Burris HA.Eur J Cancer. 2011 Oct;47(15):2256-64. doi: 10.1016/j.ejca.2011.07.008. Epub 2011 Aug 16. PMID: 21852114 3:PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. 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. doi: 10.1158/1535-7163.MCT-09-0915. Epub 2010 Mar 30. PMID: 20354118 Free Article