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12998
Vatalanib
Activators & Inhibitors
Chemical Modulators

Vatalanib #12998

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Vatalanib: Image 1
Western blot analysis of extracts from NCI-H526 cells, serum-starved overnight and untreated (-) or pretreated with Vatalanib (1000 nM, 2 hr; +) prior to treatment with Human Stem Cell Factor (hSCF) #8925 (100 ng/ml, 5 min; +), using Phospho-c-Kit (Tyr703) (D12E12) Rabbit mAb #3073 (upper) or c-Kit (D13A2) XP® Rabbit mAb #3074 (lower).
Vatalanib: Image 2
Western blot analysis of extracts from HUVE cells, serum-starved overnight and untreated (-) or pretreated with Vatalanib (1000 nM, 2 hr; +) prior to treatment with Human Vascular Endothelial Growth Factor-165 (hVEGF165) #8065 (50 ng/ml, 5 min; +), using Phospho-VEGF Receptor 2 (Tyr1175) (19A10) Rabbit mAb #2478 (upper) or VEGF Receptor 2 (55B11) Rabbit mAb #2479 (lower).
Vatalanib: Image 3
Chemical structure of vatalanib.

Product Usage Information

Vatalanib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1.19 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 0.5-50 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 72 hr.

Storage

Store lyophilized or in solution at -20ºC, desiccated. Protect from light. 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 419.73 g/mol
Purity >99%
Molecular Formula C20H15ClN4•2HCl
CAS 212141-51-0
Solubility Soluble in DMSO at 20mg/ml and H2O at 100mg/ml.

Background

Vatalanib is a multi-targeted tyrosine kinase inhibitor. Researchers performing in vitro kinase assays show that vatalanib inhibits VEGFR-1, -2, and -3 with IC50 values of approximately 77 nM, 37 nM, and 640 nM, respectively. Vatalanib also inhibited PDGFR and c-kit at sub micromolar concentrations, but had no activity against several other kinases, including c-Met, EGFR, c-Src, and v-Abl up to 10 μM (1). Vatalanib inhibits VEGF-induced autophosphorylation in HUVE and VEGFR-2 transfected CHO cells with an IC50 of 17 nM and 34 nM, respectively, and effectively blocks VEGF-stimulated HUVE cell proliferation (1). Research studies have demonstrated that vatalanib inhibits proliferation of multiple myeloma (MM) cells in a dose-dependant manner and blocks VEGF-induced ERK phosphorylation and cell migration in MM.1S cells (2). Dose-dependent apoptosis in chronic lymphocytic leukemia (CLL) cells by vatalanib and pazopanib has been observed (3).
  1. Wood, J.M. et al. (2000) Cancer Res 60, 2178-89.
  2. Lin, B. et al. (2002) Cancer Res 62, 5019-26.
  3. Paesler, J. et al. (2010) Clin Cancer Res 16, 3390-8.

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 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 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.
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
XP is a registered trademark of Cell Signaling Technology, Inc.
To Purchase # 12998
Cat. # Size Qty. Price
12998S
5 mg $ 90