Sorafenib

• 产品编号：CST-8705S      品牌：CST       原厂货号：8705S
• 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：

提供索拉非尼的冻干粉末。将其10mg重新溶解在1.57 ml DMSO中，即为10mM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。索拉非尼能以200 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10-20μM。索拉非尼也被称为Bay 43-9006，是一种新型的多激酶抑制剂，针对丝氨酸/苏氨酸激酶与酪氨酸激酶受体的RAF家族，参与肿瘤发生和肿瘤血管生成，包括：VEGFR-2 (IC50 = 90 nM), VEGFR-3 (IC50 = 20 nM), PDGFR- (IC50 = 57 nM), c-KIT (IC50 = 68 nM)和Flt3 (IC50 = 58 nM) (1)。研究表明，在一些肿瘤细胞株中，索拉非尼通过下调髓系细胞白血病抗凋亡蛋白1（Mcl-1）来诱导细胞凋亡。索拉非尼下调Mcl-1与细胞色素c从线粒体释放到细胞质中以及半胱天冬酶的激活有关，导致细胞凋亡（2）。已发现，在多种细胞类型中索拉非尼抑制STAT3（3-5）。

原厂资料：

Molecular Characterization

C21H16ClF3N4O3 • C7H8O3S

Directions for Use

Sorafenib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 10 mg in 1.57 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. Soluble in DMSO at 200 mg/ml; very poorly soluble in ethanol and water with maximum solubility in water ~10-20 µM.

Background

Sorafenib, also known as Bay 43-9006, is a novel multikinase inhibitor that targets the RAF family of serine/threonine kinases and tyrosine kinase receptors involved in tumor progression and tumor angiogenesis, including: VEGFR-2 (IC50 = 90 nM), VEGFR-3 (IC50 = 20 nM), PDGFR- (IC50 = 57 nM), c-KIT (IC50 = 68 nM), and Flt3 (IC50 = 58 nM) (1). Research studies have demonstrated that sorafenib induces apoptosis in several tumor cell lines through the down-regulation of the antiapoptotic protein myeloid cell leukemia-1 (Mcl-1). Down-regulation of Mcl-1 by sorafenib is associated with the release of cytochrome c from mitochondria into the cytosol and caspase activation, leading to apoptotic cell death (2). STAT3 inhibition by sorafenib has been observed in multiple cell types (3-5).

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