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






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。


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).


Application References

Have you published research involving the use of our products? If so we'd love to hear about it. Please let us know!

Companion Products

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.

用户评论 --- 共 0


我要参与评论 :