Pazopanib #12466

Inquiry Info. # 12466

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Product Information

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
CAS	444731-52-6
Solubility	Soluble in DMSO at 8.3mg/ml.

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).

Alternate Names

angiogenesis; c-kit; ckit; GW-786034; kit; pazopanib; PDGF; PDGR; tumor progression; VEGF; VEGFR; VEGFR1; VEGFR2; VEGFR3

Limited Uses

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For Research Use Only. Not for Use in Diagnostic Procedures.

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