产品说明
一般描述
A potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton’s Tyrosine Kinase (BTK; IC50 = 17.2 µM for human BTK in vitro and IC50 = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC50 = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.
A potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton′s tyrosine kinase (BTK; IC50 = 17.2 µM for human BTK in vitro and IC50 = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC50 = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.
包装
5 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Primary Target
Human Bruton′s Tyrosine Kinase (BTK)
Product competes with ATP.
Target IC50: 17.2 µM for human BTK in vitro and 2.5 µM for recombinant BTK
Reversible: yes
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Uckun, F.M., et al. 2006. Bioorg. Med. Chem. In press.
Mahajan, S., et al. 1999. J. Biol. Chem. 274, 9587.
Vassilev, A., et al. 1999. J. Biol. Chem. 274, 1646.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C11H8Br2N2O2 |
分子量 | 360.00 |
产品性质
质量水平 | 100 |
测定 | ≥97% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | light brown |
溶解性 | DMSO: 200 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 1 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich