Powder: -20°C for 3 years | In solvent: -80°C for 1 year
XMU-MP-3 is a robust, non-covalent inhibitor of BTK, exhibiting exceptional potency with IC50 values of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation, respectively, in the presence of 10 μM ATP. Moreover, XMU-MP-3 elicits apoptosis.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 3,330 | 5日内发货 | ||
5 mg | ¥ 3,730 | 5日内发货 | ||
25 mg | ¥ 14,700 | 6-8周 | ||
50 mg | ¥ 19,100 | 6-8周 | ||
100 mg | ¥ 29,900 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 4,730 | 5日内发货 |
产品描述 | XMU-MP-3 is a robust, non-covalent inhibitor of BTK, exhibiting exceptional potency with IC50 values of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation, respectively, in the presence of 10 μM ATP. Moreover, XMU-MP-3 elicits apoptosis. |
靶点活性 | BTK (WT):10.7 nM (IC50), BTK (C481S):17.0 nM (IC50) |
体外活性 | XMU-MP-3 (0.001-10000 nM; 48 hours) inhibits BTK-transformed Ba/F3 cell proliferation with an IC 50 of 11.4 nM[1]. XMU-MP-3 (1-10000 nM) inhibits the proliferation of JeKo-1, Ramos and NALM-6 with IC 50 values of 326.6 nM, 685.6 nM and 1065 nM, respectively[1]. XMU-MP-3 (0.001-10000 nM) maintains inhibitory potency with an IC 50 of 182.3 nM against BTK(C481S)-Ba/F3 cells[1]. XMU-MP-3 (5000 nM) induces apoptosis in BTK (C481S) Ba/F3 cells[1]. XMU-MP-3 (10-1000 nM; 4 hours) inhibits both the auto- and trans-phosphorylation of BTK at the site of Y223 and Y551 in a dose-dependent manner in BTK-transformed Ba/F3 cells[1]. Cell Proliferation Assay[1]Cell Line: BTK-transformed and parental Ba/F3 cells Concentration: 0.001, 0.01, 0.1, 1, 10, 100, 1000, 10000 nM Incubation Time: 48 hours Result: Inhibited BTK-transformed Ba/F3 cell proliferation with an IC 50 of 11.4 nM, while it showed negligible anti-proliferative effects on parental wild-type Ba/F3 cells (IC 50 >10000 nM). Western Blot Analysis[1]Cell Line: BTK-transformed Ba/F3 cells Concentration: 10, 50, 100, 500, 1000 nM Incubation Time: 4 hours Result: The phosphorylation levels of BTK Y223 and Y551 were reduced significantly at concentrations as low as 100 nM, and completely suppressed at the concentration of 1000 nM. |
体内活性 | XMU-MP-3 (25 and 50 mg/kg) substantially suppresses tumor growth in mouse xenograft models[1]. Animal Model: Nu/nu BALB/c mice (4-6 weeks of age) bearing BTK-transformed Ba/F3 and Ramos xenograft models[1]Dosage: 25 and 50 mg/kg Administration: Treated by tail vein injection; the injection volume was 0.1 mL per 10 g; daily for 14 days Result: Significantly reduced the tumor size without affecting animal weights. |
分子量 | 536.563 |
分子式 | C27H27F3N8O |
CAS No. | 2031152-08-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
XMU-MP-3 2031152-08-4 XMU MP 3 XMUMP3 Inhibitor inhibitor inhibit