产品名称

尼罗替尼(Nilotinib)

一般描述

Nilotinib(尼罗替尼) is an orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase  inhibitor with antineoplastic activity.

别 称

4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide; Tasigna; AMN107; AMN 107; UNII-F41401512X

纯 度

≥99%(HPLC)

CAS NO.

641571-10-0

分子式

C²⁸H²²F³N⁷O

分子量

529.527

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色至类白色固体

溶解性(25℃)

DMSO

≥20mg/mL

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Nilotinib is a transduction inhibitor that  targets BCR-ABL, c-kit and PDGF, for the potential treatment of various leukemias, including chronic myeloid leukemia (CML).

Nilotinib is an orally bioavailable  aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Designed to overcome imatinib resistance, nilotinib  binds to and stabilizes the inactive conformation of the kinase domain of the Abl protein of the Bcr-Abl fusion protein, resulting in the inhibition of the Bcr-Abl-mediated proliferation of Philadelphia chromosome-positive (Ph₊) chronic myeloid leukemia (CML) cells. This agent also inhibits the receptor tyrosine kinases platelet-derived growth factor receptor (PDGF-R) and c-kit, a receptor tyrosine kinase mutated and constitutively activated in most gastrointestinal stromal tumors (GISTs). With a binding mode that is energetically more favorable than that of imatinib, nilotinib has been shown to have an approximately 20-fold increased potency in kinase and proliferation assays compared to imatinib.

l  包装与存储

包 装

50mg; 500mg

存储温度

0-5℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.   https://www.ncbi.nlm.nih.gov