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CAS No.: 778270-11-4

GNF-2 Catalog No. CSN13825

Synonyms: Bcr-Abl Inhibitor

GNF-2 is a highly selective non-ATP competitive inhibitor of oncogenic Bcr-Abl activity (IC50 = 0.14 μM).

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Bcr-Abl

IC50:0.14μM
描述Bcr-Abl is a 210-kDa fusion protein with the combination of the ABL1 (Abelson tyrosine kinase) and the BCR (breakpoint cluster region) , which is validated as a therapeutic target for the treatment of chronic myelogenous leukemia. GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibited cell proliferation with an IC50 of 138 nM and cell growth with an IC50 of ~170 nM in Bcr-Abl-expressing cell lines. The cellular tyrosine phosphorylation of Bcr-Abl was inhibited by GNF-2 in a dose-dependent manner with an IC50 of 267 nM. Treatment of Ba/F3.p210 cell lines with 1 μM GNF-2 for 90min significantly decreased the level of phospho-Stat5. Incubation of 1 μM GNF-2 for 48 hours induced apoptotic death in Ba/F3.p210 (wild type and E255V mutant) cells. With the presence of c-Abl SH3 and/or SH2 domains, 10 μM GNF-2 inhibited tyrosine kinase activity of recombinant Abl in vitro. The phosphorylation of CrkII, a well-characterized c-Abl substrate, was inhibited by GNF-2 in a dose-dependent manner from 0.1 to 10 μM in one hour in c-Abl-reconstituted 3T3 cells. The combination of 5 or 10 μM GNF-2 and 1 μM imatinib decreased the number of resistant clones resulted from continuous exposure to 1 μM imatinib by 90% in Ba/F3 cells after 21-day treatment.
作用机制GNF-2 inhibits tyrosine kinase activity in c-Abl through competing with the myristoyl residue for binding to the myristate-binding pocket.
动物研究
剂量
Mice: 10 mg/kg^[4] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 10 mg/kg^[4] (i.p.)
给药途径	i.p.

[1] Adrián FJ, Ding Q, Sim T, et al. Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol. 2006;2(2):95-102.
[2] Choi Y, Seeliger MA, Panjarian SB, et al. N-myristoylated c-Abl tyrosine kinase localizes to the endoplasmic reticulum upon binding to an allosteric inhibitor. J Biol Chem. 2009;284(42):29005-14.
[3] Zhang J, Adrián FJ, Jahnke W, et al. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature. 2010;463(7280):501-6.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6715 mL
- 13.3576 mL
- 26.7151 mL
- 5 mM
- 0.5343 mL
- 2.6715 mL
- 5.3430 mL
- 10 mM
- 0.2672 mL
- 1.3358 mL
- 2.6715 mL

技术信息

CAS号

778270-11-4

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H13F3N4O2

运输

蓝冰

分子量

374.32

别名

Bcr-Abl Inhibitor

溶解度

DMSO	75 mg/ml (200.36 mM)
Water	Insoluble

动物实验配方

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