Western blot analysis of extracts from NCI-H526 cells, serum-starved overnight and untreated (-) or treated with Human Stem Cell Factor (hSCF) #8925 (100 ng/ml, 5 min; +) either with our without pazopanib pre-treatment (1 µM, 2 hr; +), using Phospho-c-Kit (Tyr703) (D12E12) Rabbit mAb #3073 (upper) or c-Kit (D13A2) XP® Rabbit mAb #3074 (lower).Learn more about how we get our images
Western blot analysis of extracts from HUVE cells, serum-starved overnight and untreated (-) or treated with Human Vascular Endothelial Growth Factor (hVEGF165) #8065 (50 ng/ml, 5 min; +) either with our without pazopanib pre-treatment (1 µM, 2 hr; +), using Phospho-VEGF Receptor 2 (Tyr1175) (19A10) Rabbit mAb #2478 (upper) or VEGF Receptor 2 (55B11) Rabbit mAb #2479 (lower).Learn more about how we get our images
Chemical structure of pazopanib.Learn more about how we get our images
Pazopanib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 10 mg in 2.29 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 0.1-10 µM for 0.5-2 hr prior to treating with a stimulator. It can also be used alone, with varying treatment times lasting up to 24 hr.
Solubility: Soluble in DMSO at 8 mg/mL with slight warming; very poorly soluble in ethanol and water with maximum in water ~10-20 µM.
Store lyophilized or in solution at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Pazopanib is a multikinase inhibitor that potently targets VEGFR1 (IC50 = 10 nM), VEGFR2 (IC50 = 30 nM), VEGFR3 (IC50 = 47 nM), PDGFRα (IC50 = 71 nM), PDGFRβ (IC50 = 84 nM), and c-Kit (IC50 = 74 nM) tyrosine kinases involved in tumor progression and angiogenesis, and can also inhibit many other tyrosine kinases at nanomolar concentrations (1). Research studies have demonstrated that pazopanib effectively blocks ligand-induced autophosphorylation of VEGFR2, PDGFRβ, and c-Kit in vitro (1,2), and selectively inhibits VEGF-induced HUVE cell proliferation over FGF (IC50 = ~21 nM vs ~720 nM). Investigators have demonstrated that pazopanib inhibits the growth, survival, and migration of multiple myeloma (MM) cell types (3).
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