Erlotinib

• 产品编号：CST-5083S      品牌：CST       原厂货号：5083S
• 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：

提供厄洛替尼的冻干粉末。将其10mg重新溶解在2.54 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 h。亦可单独使用，可采用不同的处理时间，最长达24小时。加热时，在DMSO中能以100mg/ml溶解，在水中的最大溶解度约为5-20μM。厄洛替尼是一种新的和有效的EGFR激酶通路ATP竞争性抑制剂。它在体外抑制EGFR的自磷酸化，并抑制纯化的EGFR激酶，其IC50分别为20nM和2nM（1）。厄洛替尼对EGFR的选择性比c-src和v-abl (1), ErbB-2和ErbB-4 (2)高出1000倍。有研究显示，厄洛替尼在多种细胞类型中抑制生长并诱导G1细胞周期阻滞，这些细胞有许多是过量表达EGFR（1,3-5）。

原厂资料：

Molecular Characterization

C22H23N3O4

Purity

>99%

Directions for Use

Erlotinib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 10 mg in 2.54 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 hours prior to treating with a stimulator. It can also be used alone, with varying treatment times lasting up to 24 hours. Soluble in DMSO at 100 mg/ml, soluble in ethanol at 10 mg/ml with warming; very poorly soluble in water with a maximum solubility ~5-20 µM.

Background

Erlotinib is a novel and potent ATP-competitive inhibitor of the EGFR kinase pathway. It inhibited EGFR autophosphorylation with an IC50 of 20 nM in vitro and inhibit purified EGFR kinase with an IC50 of 2 nM (1). Erlotonib is greater than 1000-fold more selective for EGFR than c-src and v-abl (1), ErbB-2, and ErbB-4 (2). Studies have shown that erlotinib inhibits growth and induces G1 cell cycle arrest in multiple cell types, many of which overexpress EGFR (1,3-5).

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