Crizotinib

• 产品编号：CST-4401S      品牌：CST       原厂货号：4401S
• 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

C21H22Cl2FN5O

Purity

>99%

提供克唑替尼的冻干粉末。将其2.5 mg重新溶解在5.55 ml DMSO中，即为1 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0.1-1 µM浓度在用刺激处理之前先预处理2-6 h。加热时，在DMSO中能以25 mg/ml溶解，微溶于水，在水中的最大溶解度约为10-20μM。克唑替尼也被称为PF-02341066，是一种新型的ATP竞争性受体激酶抑制剂，对c-Met和间变性淋巴瘤激酶（ALK）等超过120多样激酶显示出较高的特异性（1,2）。研究人员证明，克唑替尼抑制c-Met的磷酸化和c-Met依赖性增殖，体外人体肿瘤细胞的迁移和侵袭（IC50值分别为5-20nM）（1）。克唑替尼对抗组成性激活的致癌融合蛋白核磷蛋白（NPM）-ALK，抑制其磷酸化（平均IC50为24 nM），抑制细胞生长，在ALK-阳性ALCL (间变性大细胞淋巴瘤) 细胞系KARPAS-299和SU-DHL-1中诱导G1-S期细胞周期阻滞和凋亡是有效的（2）。

原厂资料：

Molecular Characterization

C21H22Cl2FN5O

Purity

>99%

Directions for Use

Crizotinib is supplied as a lyophilized powder. For a 1 mM stock, reconstitute the 2.5 mg in 5.55 ml DMSO. Working concentrations and length of treatments vary depending on the desired effect, but it is typically used at 0.1-1 µM for 2-6 h. Soluble in DMSO at 25 mg/ml with warming; very poorly soluble in water with maximum solubility ~10-20 µM.

Background

Crizotinib, also known as PF-02341066, is a novel, ATP-competitive receptor kinase inhibitor, showing high specificity for c-Met and anaplastic lymphoma kinase (ALK) over 120 other diverse kinases (1,2). Researchers have shown that crizotinib inhibits c-Met phosphorylation and c-Met-dependent proliferation, migration, and invasion of human tumor cells in vitro (IC50 values of 5–20 nM) (1). Crizotinib is effective against the constitutively active oncogenic fusion protein nucleophosmin (NPM)-ALK, inhibiting its phosphorylation (mean IC50 of 24 nM), inhibiting cell growth, and inducing G1-S phase cell cycle arrest and apoptosis in the ALK-positive ALCL (anaplastic large-cell lymphoma) cell lines KARPAS-299 and SU-DHL-1 (2).

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.