keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EEDi-5285 是一种非常有效且具有口服活性的胚胎外胚层发育 (EED) 抑制剂,结合 EED 蛋白的 IC50 值为 0.2 nM,并具有抗癌活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,890 | 现货 | ||
5 mg | ¥ 4,670 | 现货 | ||
10 mg | ¥ 6,660 | 现货 | ||
25 mg | ¥ 9,970 | 现货 | ||
50 mg | ¥ 13,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 5,170 | 现货 |
产品描述 | EEDi-5285, an orally active and highly potent inhibitor targeting embryonic ectoderm development (EED) protein, exhibits anti-cancer activity. It demonstrates exceptional efficacy with an IC50 value of 0.2 nM, indicating robust binding affinity to the EED protein. |
靶点活性 | EED:0.2 nM (IC50) |
体外活性 | EEDi-5285在携带EZH2突变的Pfeiffer和KARPAS422淋巴瘤细胞系中,分别以20 pM和0.5 nM的IC50值抑制细胞生长[1]。 |
体内活性 | EEDi-5285 (compound 28; 50-100 mg/kg; oral gavage; daily; for 28 days; SCID mice) treatment achieves complete and durable tumor regression in the KARPAS422 xenograft model in mice with oral administration. A single 100 mg/kg oral administration of EEDi-5285 (compound 28) effectively reduces the level of H3K27me3 at 24 h in KARPAS422 tumor tissue in mice. EEDi-5285 (compound 28) achieves a Cmax of 1.8 μM and an AUC of 6.0 h▪μg/ml with 10 mg/kg oral administration and has an oral bioavailability (F) of 75%. EEDi-5285 has a moderate volume of distribution of 1.4 L/kg and a terminal T1/2 of approximately 2 h[1]. |
别名 | UM-EEDi-5285, EEDI5285 |
分子量 | 479.53 |
分子式 | C24H22FN5O3S |
CAS No. | 2488952-40-3 |
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 112.5 mg/mL (234.6 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0854 mL | 10.4269 mL | 20.8538 mL | 52.1344 mL |
5 mM | 0.4171 mL | 2.0854 mL | 4.1708 mL | 10.4269 mL | |
10 mM | 0.2085 mL | 1.0427 mL | 2.0854 mL | 5.2134 mL | |
20 mM | 0.1043 mL | 0.5213 mL | 1.0427 mL | 2.6067 mL | |
50 mM | 0.0417 mL | 0.2085 mL | 0.4171 mL | 1.0427 mL | |
100 mM | 0.0209 mL | 0.1043 mL | 0.2085 mL | 0.5213 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。
EEDi-5285 2488952-40-3 Chromatin/Epigenetic Histone Methyltransferase UM-EEDi-5285 EEDI5285 EEDI 5285 Inhibitor inhibitor inhibit