Pazopanib

• 产品编号：CST-12466S      品牌：CST       原厂货号：12466S
• 产品分类：生化试剂 > 生物试剂 > 生物活性小分子 > 抑制剂
• 应用分类：

描述：

Molecular Weight:

437.52 g/mol

Molecular Characterization

 C₂₁H₂₃N₇O₂S

Purity

 >99%

原厂资料：

Molecular Weight:

437.52 g/mol

Molecular Characterization

 C₂₁H₂₃N₇O₂S

Purity

 >99%

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

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).

注意事项：

Storage: Store lyophilized or in solution at -20°C, 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