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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).

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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).

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Chemical structure of pazopanib.

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Product Usage Information

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.


Storage: 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.

Product Description

Molecular Weight:

437.52 g/mol


Purity:

>99%


Molecular Formula:

C21H23N7O2S


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).


1.  Kumar, R. et al. (2007) Mol Cancer Ther 6, 2012-21.

2.  Kumar, R. et al. (2009) Br J Cancer 101, 1717-23.

3.  Podar, K. et al. (2006) Proc Natl Acad Sci U S A 103, 19478-83.



For Research Use Only. Not For Use In Diagnostic Procedures.
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
XP is a registered trademark of Cell Signaling Technology, Inc.

12466
Pazopanib