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].\n\nA 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]\n\nChemical Name: N-Methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide\n \nSolubility: 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.\n\nStorage: Store at or below -20C.

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SPECIFICATIONS

Catalog Number

A0927-01

Size

50mg

References

^Wilmes LJ, Pallavicini MG, Fleming LM, Gibbs J, Wang D, Li KL, Partridge SC, Henry RG, Shalinsky DR, Hu-Lowe D, Park JW, McShane TM, Lu Y, Brasch RC, Hylton NM. (2007) AG-013736, a novel inhibitor of VEGF receptor tyrosine kinases, inhibits breast cancer growth and decreases vascular permeability as detected by dynamic contrast-enhanced magnetic resonance imaging. Magn Reson Imaging 25(3):319-27\n^ Rini B, Rixe O, Bukowski R, Michaelson MD, Wilding G, Hudes G, Bolte O, Steinfeldt H, Reich SD, Motzer R. (2005) AG-013736, a multi-target tyrosine kinase receptor inhibitor, demonstrates anti-tumor activity in a Phase 2 study of cytokine-refractory, metastatic renal cell cancer (RCC). ASCO Proceedings Abstract 4509\n^ Rugo HS, Herbst RS, Liu G, Park JW, Kies MS, Steinfeldt HM, Pithavala YK, Reich SD, Freddo JL, Wilding G. (2005) Phase I trial of the oral antiangiogenesis agent AG-013736 in patients with advanced solid tumors: pharmacokinetic and clinical results. J Clin Oncol. 23(24):5474-83\n^ Spano JP, Chodkiewicz C, Maurel J, Wong R, Wasan H, Barone C, L

Alternative Names

N-Methyl-2-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]benzamide; AG 013736