半岛bd体育手机客户端 说明
一般描述
A potent, reversible, cell-permeable, and ATP-competitive inhibitor of Janus protein tyrosine kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC50= 15 nM for murine JAK1), JAK2 (IC50= 1 nM), JAK3 (Ki= 5 nM), and Tyk2 (IC50= 1 nM). Inhibits other kinases at much higher concentrations. Shown to inhibit IL2- and IL4-dependent proliferation of CTLL cells and block the phosphorylation of STAT5; and further induce growth inhibition of multiple myeloma cells expressing activated JAKs and STAT3, unlike AG 490 (Cat. No. 658401). A 10 mM (500 ?g/162 ?l) solution of JAK Inhibitor I (Cat. No. 420097) in DMSO is also available.
A potent, cell-permeable, reversible, and ATP-competitive inhibitor of Janus protein tyrosine kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC50= 15 nM for murine JAK1), JAK2 (IC50= 1 nM), JAK3 (Ki= 5 nM), and Tyk2 (IC50= 1 nM). Inhibits other kinases at much higher concentrations. Shown to inhibit IL2- and IL4-dependent proliferation of CTLL cells and block the phosphorylation of STAT5, and further induce growth inhibition of multiple myeloma cells expressing activated JAKs and STAT3, unlike AG 490 (Cat. No. 658401).
包装
500 μg in Plastic ampoule
1 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Target Ki: 5 nM against JAK3
Target IC50: 15 nM against murine JAK1; 1 nM against JAK2; 1 nM against Tyk2
Reversible: yes
Cell permeable: yes
Primary Target
murine JAK1
Product competes with ATP.
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
Pedranzini, L., et al. 2006.Cancer Res.66,9714.
Lucet, I.S., et al. 2005.Blood107,176.
Thompson, J.E., et al. 2002.Bioorg. Med. Chem. Lett.12,1219.
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 | C18H16FN3O |
分子量 | 309.34 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze protect from light |
颜色 | off-white |
溶解性 | DMSO: 5 mg/mL |
运输 | ambient |
储存温度 | ?20℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |