Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK778 是BET 蛋白BD1溴结构域的选择性抑制剂,对BRD2 BD1、BRD3 BD1、BRD4 BD1、BRDT BD1的IC50分别为75 nM,41 nM,41 nM 和143 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,650 | 现货 | ||
5 mg | ¥ 3,290 | 现货 | ||
10 mg | ¥ 5,290 | 现货 | ||
25 mg | ¥ 7,830 | 现货 | ||
50 mg | ¥ 10,700 | 现货 | ||
100 mg | ¥ 14,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 150 | 现货 |
产品描述 | GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis. |
靶点活性 | BRD3 BD1:41 nM, BRD2 BD1:75 nM, BRDT BD1:143 nM, BRD4 BD1:41 nM |
体外活性 | GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. GSK778 inhibits BRD BD2 receptors such as BRD2 BD2 (IC50 = 3950 nM), BRD3 BD2 (IC50 = 1210 nM ), BRD4 BD2 (IC50 = 5843 nM), and BRDT BD2 (IC50 = 17451 nM)[1]. GSK778 (0.001-10 μM; 5 days) has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells. GSK778 (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML cells. GSK778 (0.01-10 μM; 72 hours) inhibited the production of effector cytokines including IFNγ, IL-17A and IL-22 and the proliferative activity of human primary CD4+ T cells[1]. |
体内活性 | GSK778 (15?mg/kg/BID; s.c. for 14 days) reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM and is well tolerated[1]. GSK778 (15?mg/kg/BID; i.p. for 30 days) offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model[1]. The Cmax, Tmax and AUC∞ values are 85 ng/mL, 1.48 h and 132 ng.h/mL, respectively. |
分子量 | 511.61 |
分子式 | C30H33N5O3 |
CAS No. | 2451862-42-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 41.67 mg/mL (81.45 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9546 mL | 9.7731 mL | 19.5461 mL | 48.8653 mL |
5 mM | 0.3909 mL | 1.9546 mL | 3.9092 mL | 9.7731 mL | |
10 mM | 0.1955 mL | 0.9773 mL | 1.9546 mL | 4.8865 mL | |
20 mM | 0.0977 mL | 0.4887 mL | 0.9773 mL | 2.4433 mL | |
50 mM | 0.0391 mL | 0.1955 mL | 0.3909 mL | 0.9773 mL |
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。
GSK778 2451862-42-1 Chromatin/Epigenetic Epigenetic Reader Domain iBET-BD1 GSK 778 GSK-778 Apoptosis inhibit Inhibitor inhibitor