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12466
Pazopanib
Activators & Inhibitors
Chemical Modulators

Pazopanib #12466

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Pazopanib: Image 1
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).
Pazopanib: Image 2
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).
Pazopanib: Image 3
Chemical structure of pazopanib.

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).
  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.

Limited Uses

Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.

Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST's products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST's Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

For Research Use Only. Not For Use In Diagnostic Procedures.
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XP is a registered trademark of Cell Signaling Technology, Inc.
To Purchase # 12466
Cat. # Size Qty. Price
12466S
10 mg $ 142