Lapatinib

• 产品编号：CST-12121S      品牌：CST       原厂货号：12121S
• 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：

提供拉帕替尼的冻干粉末。将其10mg重新溶解在1.08 ml DMSO中，即为10 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72小时。拉帕替尼是一种EGFR和HER2受体酪氨酸激酶的双重抑制剂（1-4）。研究表明，在无细胞激酶检测中，拉帕替尼抑制纯化的EGFR和HER2酪氨酸激酶结构域，IC50值分别为10.8 nM和9.2 nM，抑制HER4的IC50为367 nM。在这些检测分析中，拉帕替尼比许多其他激酶包括C-SRC，MEK，ERK和p38，对HER2和EGFR的选择性大300多倍（1）。有研究表明，在过表达这些激酶的细胞类型中，拉帕替尼有效地抑制EGFR和HER2受体的自身磷酸化，细胞生长抑制与HER2过表达有关（2-4）。

原厂资料：

Molecular Characterization

C29H26ClFN4O4S•2C7H8O3S

Purity

>99%

Directions for Use

Lapatinib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 10 mg in 1.08 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but is typically used at 0.1-10 µM either as a pretreatment for 0.5-2 hr prior to treating with a stimulator or used alone with varying treatment times lasting up to 72 hr.

Background

Lapatinib is a dual inhibitor of EGFR and HER2 tyrosine kinases (1-4). Researchers have shown that lapatinib inhibits purified EGFR and HER2 tyrosine kinase domains in cell-free kinase assays with IC50 values of 10.8 nM and 9.2 nM, respectively, and HER4 with an IC50 of 367 nM. Lapatinib was greater than 300-fold more selective for HER2 and EGFR than many other kinases, including c-src, MEK, Erk, and p38 in these assays (1). Studies have shown that lapatinib effectively inhibits both EGFR and HER2 autophosphorylation in cell types over expressing these kinases, and cell growth inhibition is correlated with HER2 overexpression (2-4).

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.