Axitinib (AG 013736)

InformationAxitinib (AG 013736) is a multi-target inhibitor ofVEGFR1,VEGFR2,VEGFR3, PDGFRβ and c-Kit withIC50of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.In vitroAxitinib could block the cellular autophosphorylation of VEGFR and VEGF-mediated endothelial cell viability, tube formation, and downstream signaling. Axitinib inhibits the proliferation of variable cell lines with IC50 of >10,000 nM (IGR-N91), 849 nM (IGR-NB8), 274 nM (SH-SY5Y) and 573 nM (non-VEGF stimulated HUVEC).In vivoAxitinib exhibits primary inhibition to orthotopically transplanted models such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). Axitinib delays the tumor growth with 11.4 days compared to the controls (p.o. 30 mg/kg) and decreases the Mean Vessels Density (MVD) to 21, compared to 49 in controls, in IGR-N91 flank xenografts. Axitinib significantly inhibits growth and disrupts tumor microvasculature in BT474 breast cancer model at 10-100 mg/kg. Axitinib has shown single-agent activity in variable tumors, including renal cell carcinoma, thyroid cancer, non-small cell lung cancer, and melanoma.Cell Datacell lines：DLBCL cells, SUDHL-6 cellsConcentrations：1 nM - 10 μMIncubation Time：72 hoursPowder Purity:≥99%.

Specifications and Purity: 10mM in DMSO

Molecular Formula: C22H18N4OS

Molecular Weight: 386.47

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