Nilotinib

• 产品编号：CST-12209S      品牌：CST       原厂货号：12209S
• 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：

提供尼洛替尼的冻干粉末。将其5mg重新溶解在1.89 ml DMSO中，即为5 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10-1000 nM浓度在用刺激处理之前先预处理2-72 hr. 尼洛替尼能以50 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。尼洛替尼（AMN-107）是一种新型的酪氨酸激酶抑制剂，能有效地抑制Bcr-Abl。比伊马替尼，尼洛替尼更有效降低表达野生型Bcr-Abl的细胞的增殖和活力，并积极对抗除了T315I的许多伊马替尼耐药的Bcr-Abl突变（1-4）。已证明，尼罗替尼在表达野生型Abl的细胞中和伊马替尼耐药突变Abl的细胞中，尼罗替尼有效抑制Abl活性比伊马替尼高20倍。尼罗替尼在抑制Abl的自身磷酸化时是同样有效的（3）。调查研究表明，尼洛替尼处理的表达Bcr-Ab的K-562细胞Stat5和CrkL的磷酸化衰减，降低Bcl-xL和c-Myc的表达，诱导p27和Bim表达，诱导PARP裂解。与组蛋白去乙酰化酶抑制剂LBH589协同处理，许多这些效果会增强（5）。

原厂资料：

Directions for Use

Nilotinib is supplied as a lyophilized powder. For a 5 mM stock, reconstitute the 5 mg in 1.89 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 10-1000 nM for 2-72 hr. Nilotinib is soluble in DMSO at 50 mg/ml; very poorly soluble in ethanol and water with maximum solubility in water at ~10-20 µM.

Background

Nilotinib (AMN-107) is a novel tyrosine kinase inhibitor that potently inhibits Bcr-Abl. Nilotinib is more effective than imatinib at decreasing the proliferation and viability in cells expressing wild-type Bcr-Abl and is active against many imatinib-resistant Bcr-Abl mutants, with the exception of T315I (1-4). Nilotinib has been shown to inhibit Abl activity in cells expressing wild-type Abl and imatinib-resistant mutant Abl, with ~20-fold greater potency than imatinib. Nilotinib is similarly effective at inhibiting Abl autophosphorylation (3). Research studies have demonstrated that nilotinib treatment of Bcr-Abl-expressing K-562 cells attenuates Stat5 and CrkL phosphorylation, decreases Bcl-xL and c-Myc expression, induces p27 and Bim expression, and induces PARP cleavage. Many of these effects are enhanced by cotreatment with the histone deacetylase inhibitor LBH589 (5).

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.