AG013736 (Axitinib)

Axitinib (also known as AG013736) is a small molecule tyrosine kinase inhibitor under development by Pfizer. It inhibits multiple targets, including VEGFR-1, VEGFR-2, VEGFR-3, platelet derived growth factor receptor (PDGFR), and cKIT (CD117). It has been shown to significantly inhibit growth of breast cancer in xenograft models [1] and has been successful in trials with renal cell carcinoma (RCC) [2] and several other tumor types [3]. A Phase II clinical trial showed good response in combination chemotherapy with Gemcitabine for advanced pancreatic cancer[4]. However, Pfizer reported on January 30, 2009 that Phase III clinical trials of the drug when used in combination with Gemcitabine showed no evidence of improved survival rates over treatments using Gemcitabine alone for advanced pancreatic cancer and halted the trial. [1] , Chemical Name: N-Methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide, , Solubility: Soluble in DMSO at 33mg/ml, soluble in ethanol at 1.7mg/ml with warming, very poorly soluble in water, maximum solubility in plain water is estimated to be about 10-50uM, buffers, serum, or other additives may increase or decrease the aqueous solubility., , Storage: Store at or below -20ºC.