Gefitinib

• 产品编号：CST-4765S      品牌：CST       原厂货号：4765S
• 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：

Molecular Characterization

C22H24ClFN4O3

Purity

>99%

提供吉非替尼的冻干粉末。将其10mg重新溶解在2.24 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24小时。吉非替尼能以100 mg/ml溶解在DMSO中，非常难溶于乙醇和水。吉非替尼是一种新的有效的表皮生长因子受体酪氨酸激酶抑制剂，结合酶的ATP-结合位点，并已被证明与肽底物具有ATP竞争性和非竞争性（1）。吉非替尼在体外抑制EGFR的活性（IC50= 33nM），当与缺乏EGF（IC50=8.8μM）时相比，显着地抑制EGF刺激的肿瘤细胞生长（IC 50=54nM），并在肿瘤细胞有效地阻止EGF的刺激自身磷酸化。与FGF-或VEGF-刺激的生长相比，它也选择性地抑制EGF刺激的HUVE细胞的生长（1）。虽然研究证明吉非替尼对于EGFR比HER2有更高的选择性（1,2），但在许多HER2过度表达的细胞系中，它也显示出抑制HER2的生长和磷酸化。

原厂资料：

Molecular Characterization

C22H24ClFN4O3

Purity

>99%

Directions for Use

Gefinitib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 10 mg in 2.24 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 100 mg/ml; very poorly soluble in ethanol and water.

Background

Gefitinib is a novel and potent EGFR tyrosine kinase inhibitor that binds to the ATP-binding site of the enzyme, and has been shown to be competitive with ATP and noncompetitive with peptide substrates (1). Gefitinib inhibits in vitro EGFR activity (IC50 = 33 nM), significantly inhibits EGF-stimulated tumor cell growth (IC50 = 54 nM) when compared to the absence of EGF (IC50 = 8.8 µM), and effectively blocks EGF-stimulated autophosphorylation in tumor cells. It also selectively inhibits EGF-stimulated growth of HUVE cells compared with FGF- or VEGF-stimulated growth (1). Although studies demonstrate gefitinib to be much more selective for EGFR than HER2 (1,2), it has also shown to inhibit growth and phosphorylation of HER2 in numerous HER2-overexpressing cell lines (3).

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