Publications
Below is a representative list of peer reviewed manuscript publications that have resulted from Ambit’s proprietary research and development programs or through collaborations with other biotechnology or pharmaceutical companies, or academic collaborators. Depending on the article, a journal subscription may be required to view the full article.
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Transient exposure to quizartinib mediates sustained inhibition of FLT3 signaling while specifically inducing apoptosis in FLT3-activated leukemia cells. Gunawardane et al. Mol Cancer Ther. 2013. In press, published online February 14, 2013.
Discovery of AC710, a globally selective inhibitor of platelet-derived growth factor receptor-family Kinases. G. Liu et al. ACS Med. Chem. Lett. 2012, 3, 997−1002.
Discovery of highly potent and selective pan-aurora kinase Inhibitors with enhanced in vivo antitumor therapeutic index. G. Liu et al. J. Med. Chem. 2012, 55, 3250−3260.
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious Inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E. Rowbottom et al. J Med Chem. 2012 Feb 9;55(3):1082-105
CEP-32496: A novel orally Active BRAFV600E inhibitor with selective cellular and in vivo antitumor activity. James et al. Mol Cancer Ther Published OnlineFirst February 7, 2012
4-quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors. Holladay, M.W. et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5342-6. Epub 2011 Jul 14.
Novel series of pyrrolotriazine analogs as highly potent pan-aurora kinase inhibitors. S. Abraham et al. Bioorg. Med. Chem. Lett. 2011, 21, 5296–5300.
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Zarrinkar, P.P. et al. Blood, October 14, 2009, 114(14):2984-92
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N’-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. Chao, Q. et al. Med Chem. 2009 Dec 10;52(23):7808-16.
Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors. Patel, H.K. et al. Bioorganic & Medicinal Chemistry Letters, July 9, 2009 5182-5185