store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GNE-781 是一种具有口服活性的选择性 CBP 抑制剂,在 TR-FRET 实验中 IC50为 0.94 nM。它还抑制BRET 和BRD4 (1),IC50分别为 6.2 和 5100 nM,有抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,160 | 现货 | ||
5 mg | ¥ 2,660 | 现货 | ||
10 mg | ¥ 3,930 | 现货 | ||
25 mg | ¥ 6,420 | 现货 | ||
50 mg | ¥ 8,780 | 现货 | ||
100 mg | ¥ 11,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,970 | 现货 |
产品描述 | GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively). |
靶点活性 | BRD41:5100 nM, CBP:0.94 nM, BRET:6.2 nM |
体外活性 | GNE-781 decreases FOXP3 (forkhead box P3) transcript levels. GNE-781 is a highly advanced potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element-binding protein, binding protein. GNE-781 is exquisitely selective for CBP/P300 and is remarkably selective for CBP (5425-fold) and P300 (4250-fold), which is shown by an examination of a subset of bromodomains. GNE-781 displays an appropriate balance of cell potency, selectivity (5425-fold over BRD4(1)) [1]. |
体内活性 | GNE-781 is a highly potent and selective inhibitor of CBP that is efficacious in a MOLM-16 AML xenograft model. GNE-781 shows antitumor activity in an AML tumor model and is also shown to reduce Foxp3 transcript levels in a dose-dependent manner and it also shows moderate to low clearance in vivo in all species evaluated, with acceptable oral bioavailability. The effect of GNE-781 is determined in an in vivo PK/PD experiment using a MOLM-16 (adult AML cell line) xenograft mouse model. GNE-781(3 and 30 mg/kg; Single doses) are given in MOLM-16 tumor-bearing animals, and samples are collected at time points covering 2-24 h. Upon tumor establishment, Administration with GNE-781(3-30 mg/kg; twice daily ). Single-agent efficacy is observed at all doses, as evidenced by inhibition of MOLM-16 tumor growth. Tumor growth inhibition (%TGI) is 73%, 71%, and 89% at 3, 10, and 30 mg/kg, respectively. All doses of GNE-781 are well tolerated over the 21-day dosing window, with a maximal body weight loss of 3.7%. Tumor RNA is generated and used to assess MYC transcript by quantitative RT-PCR relative to vehicle-treated animals. At doses as low as 3 mg/kg at 2 and 8 h, suppression of MYC is observed, with maximal suppression observed at 10 and 30 mg/kg at 2 h (87% and 88% inhibition, respectively). To evaluate the in vivo efficacy of GNE-781, MOLM-16 AML xenografts are established in SCID beige mice[1]. |
分子量 | 525.59 |
分子式 | C27H33F2N7O2 |
CAS No. | 1936422-33-1 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 95 mg/mL (180.75 mM), Sonification is recommended.
Ethanol: 95 mg/mL (180.75 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.9026 mL | 9.5131 mL | 19.0262 mL | 47.5656 mL |
5 mM | 0.3805 mL | 1.9026 mL | 3.8052 mL | 9.5131 mL | |
10 mM | 0.1903 mL | 0.9513 mL | 1.9026 mL | 4.7566 mL | |
20 mM | 0.0951 mL | 0.4757 mL | 0.9513 mL | 2.3783 mL | |
50 mM | 0.0381 mL | 0.1903 mL | 0.3805 mL | 0.9513 mL | |
100 mM | 0.019 mL | 0.0951 mL | 0.1903 mL | 0.4757 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。
GNE-781 1936422-33-1 Chromatin/Epigenetic Epigenetic Reader Domain Histone Acetyltransferase Inhibitor HATs HAT inhibit GNE781 GNE 781 inhibitor