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.
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
Holladay, M.W. et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5342-6. Epub 2011 Jul 14.
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
Phase I safety, pharmacokinetic and pharmacodynamic trial of BMS-599626 (AC480), an oral pan-HER receptor tyrosine kinase inhibitor, in patients with advanced solid tumors. Soria, J-C., et al. Annals of Oncology, May 16, 2011.
Discovery and Preclinical Evaluation of [4-[[1-(3-fluorophenyl) methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic Acid, (3S)-3-Morpholinylmethyl Ester (BMS-599626), a Selective and Orally Efficacious Inhibitor of Human Epidermal Growth Factor Receptor 1 and 2 Kinases. Gavai, A.V. et al. Journal of Medicinal Chemistry - Letter. July 8, 2009.
Preclinical Antitumor Activity of BMS-599626, a pan-HER Kinase Inhibitor that Inhibits HER1/HER2 Homodimer and Heterodimer Signaling. Wong, T.W. et al. Clinical Cancer Research, October 15, 2006. 12(20)