PF 03814735

Based on 15 reference(s) in Google Scholar 8 10 15

Axon 2023

CAS [942487-16-3]

MF C23H25F3N6O2
MW 474.48

Purity: 98%
Optical purity: Optically pure
Soluble in DMSO

PF 03814735

Description

Potent, orally bioavailable, ATP-competitive and reversible inhibitor of aurora kinase A (IC50: 0.8 nM) and aurora kinase B (IC50: 5 nM) with potential antineoplastic activity; PF 03814735 also inhibits Flt1, FAK and TrkA with IC50 values of 10, 22, 30 nM respectively; clinical candidate.

JP Jani et al. PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. Mol. Cancer Ther. 2010, 9(4), 883-894.

P Schöffski et al. Phase I, open-label, multicentre, dose-escalation, pharmacokinetic and pharmacodynamic trial of the oral aurora kinase inhibitor PF-03814735 in advanced solid tumours. Eur. J. Cancer. 2011, 47(15), 2256-2264.

KE Hook et al. An integrated genomic approach to identify predictive biomarkers of response to the aurora kinase inhibitor PF-03814735. Mol. Cancer Ther. 2012, 11(3), 710-719.

Cell Cycle Regulation Cell Signaling & Oncology Epigenetics VEGFR FAK EC 2.7.11.1 Aurora Trk Pfizer Licensed Products

ATP-competitive inhibitor of aurora kinase A and B

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

Source information

Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.

Parent CAS No.

[942487-16-3]

产品资料