store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SGC0946是一种组蛋白甲基转移酶DOT1L 高选择性抑制剂,IC50值为0.3nM,可选择性地杀死混合谱系白血病细胞。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 432 | 现货 | ||
5 mg | ¥ 778 | 现货 | ||
10 mg | ¥ 1,258 | 现货 | ||
50 mg | ¥ 2,850 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 974 | 现货 |
产品描述 | SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells. |
靶点活性 | DOT1L:0.3 nM |
体内活性 | SGC 0946可使A431细胞(IC50:2.6 nM)和MCF10A细胞(IC50:8.8 nM)中H3K79二甲基化显著降低,并可有效并选择性地杀死含MLL易位的细胞。与其类似物EPZ004777相比,SGC 0946对DOT1L更有效,从而用于癌症治疗的研究中。SGC 0946比其他组蛋白甲基转移酶/HMTs选择性高100倍。 |
激酶实验 | Determination of Inhibitor IC50 Values: EPZ004777 is serially diluted 3-fold in DMSO for a total of ten concentrations, beginning at 1 mM. A 1 μL aliquot of each inhibitor dilution is plated in a 384-well microtiter plate. The 100% inhibition control consisted of 2.5 mM ?nal concentration of the product inhibitor S-adenosyl-L-homocysteine, (SAH). Compound is incubated for 30 min with 40 ml per well of 0.25 nM DOT1L(1-416) in assay buffer (20 mM TRIS [pH 8.0] 10 mM NaCl, 0.002% Tween 20, 0.005% Bovine Skin Gelatin, 100 mM KCl, and 0.5 mM DTT). 10 ml per well of substrate mix comprising assay buffer with 200 nM 3H-SAM (American Radiolabeled Chemicals: 80 Ci/mmol), 600 nM unlabeled SAM, and 20 nM nucleosomes are added to initiate the reaction (both substrates are present in the ?nal reaction mixture at their respective KM values). Reactions are incubated for 120 min and quenched with 10 ml per well of 800 mM SAM. Incorporation of radioactivity into nucleosome substrate is measured in a ?ashplate. IC50 values for enzymes in the histone methyltransferase panel are determined under similar balanced assay conditions with both SAM and protein/peptide substrate present at concentrations equal to their respective KM values. |
化合物与蛋白结合的复合物 |
CamA Adenine Methyltransferase Complexed to Cognate Substrate DNA and Inhibitor SGC0946 |
分子量 | 618.57 |
分子式 | C28H40BrN7O4 |
CAS No. | 1561178-17-3 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
5% DMSO+95% Saline: 4.65 mg/mL (7.52 mM, suspension)
DMSO: 93 mg/mL (150.3 mM)
Ethanol: 93 mg/mL (150.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
5% DMSO+95% Saline / DMSO / Ethanol | 1 mM | 1.6166 mL | 8.0832 mL | 16.1663 mL | 40.4158 mL |
5 mM | 0.3233 mL | 1.6166 mL | 3.2333 mL | 8.0832 mL | |
DMSO / Ethanol | 10 mM | 0.1617 mL | 0.8083 mL | 1.6166 mL | 4.0416 mL |
20 mM | 0.0808 mL | 0.4042 mL | 0.8083 mL | 2.0208 mL | |
50 mM | 0.0323 mL | 0.1617 mL | 0.3233 mL | 0.8083 mL | |
100 mM | 0.0162 mL | 0.0808 mL | 0.1617 mL | 0.4042 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。
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