Sunitinib

• 产品编号：CST-12328S      品牌：CST       原厂货号：12328S
• 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：

提供舒尼替尼的冻干粉末。将其10mg重新溶解在3.76 ml DMSO中，即为5 mM储存液。工作浓度和处理时间可以根据预期的效应而改变，但通常使用0.1-10 µM浓度在用刺激剂处理之前先预处理0.5-2 hr，或单独使用具有不同处理时间，最长达24小时。舒尼替尼能以40 mg/ml溶解在DMSO中，非常难溶于乙醇和水，在水中的最大溶解度约为10-50μM。舒尼替尼也被称为SU11248，是广为人知的PDGFR，VEGFR，KIT和FLT3靶点的多种酪氨酸激酶抑制剂，因此具有抗肿瘤和抗血管生成的活性。细胞磷酸化分析显示，舒尼替尼能在纳摩尔浓度有效地抑制这些受体酪氨酸激酶的配体依赖性磷酸化，并且还可以抑制配体依赖性的细胞增殖（1-3）。 舒尼替尼显示对PDGFRB和VEGFR的选择性超过许多其他激酶10倍，包括EGFR，Cdk2，Met，IGF-1R，Abl和Src（2）。也观察到通过舒尼替尼抑制CSF-1（4）和RET（5）。

原厂资料：

Molecular Characterization

C22H27FN4O2•C4H6O5

Purity

>99%

Directions for Use

Sunitinib is supplied as a lyophilized powder. For a 5 mM stock, reconstitute the 10 mg in 3.76 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 0.1-10 µM either as a pretreatment for 0.5-2 hr prior to treating with a stimulator or is used alone with varying treatment times lasting up to 24 hr. Sunitinib is soluble in DMSO at 40 mg/ml; poorly soluble in ethanol and water with maximum solubility in water ~10-50 µM.

Background

Sunitinib, also known as SU11248, is a multi-tyrosine kinase inhibitor widely known to target PDGFR, VEGFR, KIT, and FLT3, and therefore has both antitumor and antiangiogenic activities. Cellular phosphorylation assays show that sunitinib effectively inhibits ligand-dependent phosphorylation of these receptor tyrosine kinases in nanomolar concentrations and can also inhibit ligand-dependent cellular proliferation (1-3). Sunitinib displays greater than 10-fold selectively for PDGFRB and VEGFR over numerous other kinases, including EGFR, Cdk2, Met, IGF -1R, Abl, and src (2). Inhibition of CSF-1 (4) and RET (5) by sunitinib has also been observed.

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.