Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 913 | 6-8周 | ||
5 mg | ¥ 1,720 | 6-8周 | ||
25 mg | ¥ 7,690 | 6-8周 | ||
50 mg | ¥ 9,990 | 6-8周 | ||
100 mg | ¥ 15,800 | 6-8周 |
产品描述 | GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300. |
靶点活性 | BRD4:13 μM, CBP:0.02 μM, EP300:0.03 μM |
体外活性 | GNE-272 does not inhibit any target at >30% when tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel. GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. The compound has good potency in the BRET cellular assay. GNE-272 is shown to inhibit the expression of MYC10 (MV4?11 cell line) (EC50: 0.91 μM) and a good correlation between the BRET and MYC cellular assays is observed. |
体内活性 | GNE-272 displays a marked antiproliferative effect in hematologic cancer cell lines. Which modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model. GNE-272 shows low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound Cmax of 26 μM. |
分子量 | 424.47 |
分子式 | C22H25FN6O2 |
CAS No. | 1936428-93-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (235.59 mM), Sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3559 mL | 11.7794 mL | 23.5588 mL | 58.897 mL |
5 mM | 0.4712 mL | 2.3559 mL | 4.7118 mL | 11.7794 mL | |
10 mM | 0.2356 mL | 1.1779 mL | 2.3559 mL | 5.8897 mL | |
20 mM | 0.1178 mL | 0.589 mL | 1.1779 mL | 2.9448 mL | |
50 mM | 0.0471 mL | 0.2356 mL | 0.4712 mL | 1.1779 mL | |
100 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.589 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-272 1936428-93-1 Chromatin/Epigenetic Epigenetic Reader Domain GNE 272 GNE272 Inhibitor inhibitor inhibit