Axitinib, Free Base ( AG-013736, Inlyta, CAS 319460-85-0), >99%

LC Laboratories' Product Number A-1107 - Axitinib, Free Base ( AG-013736, Inlyta, CAS 319460-85-0), >99% - for research use only. Axitinib (AG-013736) is an oral, potent, and selective inhibitor of vascular endothelial growth factor receptors 1 (VEGFR-1), 2 (VEGFR-2), and 3 (VEGFR-3), platelet derived growth factor receptor (PDGFR), and cKIT (CD117). Axitinib inhibited growth of breast tumors in vivo at doses of 10-100 mg/kg and disrupted tumor microvasculature as measured by dynamic contrast-enhanced MRI. Regrowth of blood vessels in spontaneous RIP-Tag2 tumors and implanted Lewis lung carcinomas in mice was studied after being treated with axitinib or AG-028262 for 7 days. Both agents inhibited 50%-60% of tumor neovasculature formation. Empty sleeves of basement membrane were left behind and surviving pericytes had less α-SMA immunoreactivity. Endothelial sprouts grew into empty sleeves of basement membrane one day after drug withdrawal, which was followed by vessel patency and connection to the bloodstream. Tumors were fully revascularized and the pericyte phenotype returned to baseline by 7 days. Axitinib inhibited angiogenesis significantly in rat 9L tumors grown s.c. in scid mice but only delayed tumor growth moderately. A combination of axitinib with metronomic cyclophosphamide completely blocked 9L tumor growth on initiation of drug treatment. However, metronomic cyclophosphamide alone required multiple treatment cycles to inhibit tumor growth. Axitinib has clinical activity in patients with cytokine-refractory metastatic renal-cell cancer.

• Supplier: LC Laboratories
• Product #: A-1107
• Sku #: A-1107_2g