Cell Signaling Technology

Product Pathways - Tyrosine Kinase / Adaptors

Nilotinib #12209

AMN-107   Bcr-Abl inhibitor   imatinib   K-562 cells   LBH589  

Applications Dilution Species-Reactivity Sensitivity MW (kDa) Isotype

Species cross-reactivity is determined by western blot.

Applications Key:

Molecular Characterization

C28H22F3N7O

Purity

>99%

Structure

Structure

Chemical structure of nilotinib.尼罗替尼的化学结构。

Western Blotting

Western Blotting

Western blot analysis of extracts from K-562 cells, untreated (-) or treated (+) with Nilotinib (1000 nM, 24 hr), using PathScan® Bcr/Abl Activity Assay: Phospho-c-Abl, Phospho-Stat5, and Phospho-CrkL Multiplex Western Detection Cocktail #5300 to detect inhibition of phospho-Bcr-Abl, phospho-Stat5, and phospho-CrkL.Western blot方法检测K-562细胞提取物,细胞不处理(-)或用尼罗替尼(1000 nM, 24 hr)处理(+),使用PathScan Bcr/ Abl活性分析:磷酸化c-Abl,磷酸化Stat5和磷酸化CrkL的多重Western检测混合物#5300,以检测对磷酸化Bcr-Abl,磷酸化Stat5,磷酸化CrkL的抑制。

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.

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。

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).

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)。

Application References

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For Research Use Only. Not For Use In Diagnostic Procedures.

Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.

PathScan is a trademark of Cell Signaling Technology, Inc.

Cell Signaling Technology® is a trademark of Cell Signaling Technology, Inc.

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