Background
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).
Molecular Formula
C21H23N7O2S
Molecular Weight
437.52 g/mol
Purity
>99%
CAS
444731-52-6
Solubility
Soluble in DMSO at 8.3mg/ml.
Storage
Directions for Use
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.
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
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