Vatalanib

• 产品编号：CST-12998S      品牌：CST       原厂货号：12998S
• 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：

Description

Molecular Weight:

419.73 g/mol

Molecular Characterization

C₂₀H₁₅ClN₄•2HCl

Purity

>99%

Bioactivity

Solubility: Soluble in DMSO at 10 mg/ml with warming. Very poorly soluble in ethanol. Soluble in water at 100 mg/ml.

原厂资料：

Molecular Weight:

419.73 g/mol

Molecular Characterization

C₂₀H₁₅ClN₄•2HCl

Purity

>99%

Bioactivity

Solubility: Soluble in DMSO at 10 mg/ml with warming. Very poorly soluble in ethanol. Soluble in water at 100 mg/ml.

Directions for Use

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.

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).

注意事项：

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