Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Domatinostat (4SC202) 是一种 I 型 HDAC 抑制剂,能够抑制 HDAC1、HDAC2和 HDAC3 的活性,IC50值分别为 1.20 μM、1.12 μM 和 0.57 μM,同时能够抑制组蛋白赖氨酸特异性脱甲基酶1 的活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 322 | 现货 | ||
2 mg | ¥ 463 | 现货 | ||
5 mg | ¥ 689 | 现货 | ||
10 mg | ¥ 1,120 | 现货 | ||
25 mg | ¥ 2,080 | 现货 | ||
50 mg | ¥ 3,380 | 现货 | ||
100 mg | ¥ 5,390 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 773 | 现货 |
产品描述 | Domatinostat (4SC202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1. |
靶点活性 | HDAC1:1.20 μM, HDAC3:0.57 μM, HDAC2:1.12 μM |
体外活性 | In HeLa cells, 4SC-202 induces hyperacetylation of histone H3 with EC50 of 1.1 μM. 4SC-202 induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM. [1] |
体内活性 | In vivo, 4SC-202 has a high oral bioavailability, and shows high metabolic stability and a low plasma clearance. 4SC-202 (120 mg/kg p.o.) shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model. [1] |
别名 | 4SC202, 4SC 202, 4SC-202 (free base), 4SC-202 |
分子量 | 447.51 |
分子式 | C23H21N5O3S |
CAS No. | 910462-43-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 82 mg/mL (183.2 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2346 mL | 11.1729 mL | 22.3459 mL | 55.8647 mL |
5 mM | 0.4469 mL | 2.2346 mL | 4.4692 mL | 11.1729 mL | |
10 mM | 0.2235 mL | 1.1173 mL | 2.2346 mL | 5.5865 mL | |
20 mM | 0.1117 mL | 0.5586 mL | 1.1173 mL | 2.7932 mL | |
50 mM | 0.0447 mL | 0.2235 mL | 0.4469 mL | 1.1173 mL | |
100 mM | 0.0223 mL | 0.1117 mL | 0.2235 mL | 0.5586 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。
Domatinostat 910462-43-0 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair HDAC 4SC202 inhibit 4SC 202 4SC-202 (free base) 4SC-202 Inhibitor Histone deacetylases inhibitor