Powder: -20°C for 3 years | In solvent: -80°C for 1 year
HDAC-IN-57 是一种具有口服活性的组蛋白脱乙酰酶 (HDAC) 泛抑制剂,对 HDAC1, HDAC2, HDAC6, HDAC8 具有抑制作用, IC50 值分别为 2.07 nM, 4.71 nM, 2.4 nM 和 107 nM。HDAC-IN-57 对 LSD1具有抑制作用, IC50 值为 1.34 μΜ。HDAC-IN-57 具有抗肿瘤活性,可诱导凋亡 (apoptosis)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,300 | 现货 | ||
5 mg | ¥ 2,900 | 现货 | ||
10 mg | ¥ 4,290 | 现货 | ||
25 mg | ¥ 6,850 | 现货 | ||
50 mg | ¥ 9,270 | 现货 | ||
100 mg | ¥ 12,500 | 现货 | ||
500 mg | ¥ 24,800 | 现货 |
产品描述 | HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively. HDAC-IN-57 inhibits LSD1 with an IC50 value of 1.34 μΜ. HDAC-IN-57 has anti-tumor activity and can induce apoptosis. |
靶点活性 | HDAC1:2.07 nM, HDAC2:4.71 nM, HDAC6:2.4 nM, HDAC8:107 nM |
体外活性 |
HDAC-IN-57 (Compound 5e) (1.0 μM, 2.5 μM, 5.0 μM; 48 h) effectively suppresses the migration and invasion of solid tumor cell lines, namely MGC-803, A549, and HCT-116. Furthermore, HDAC-IN-57 demonstrates significant growth inhibition in these solid tumor cell lines, exhibiting IC50 values of 0.45 μM, 1.48 μM, and 0.57 μM, respectively. Additionally, HDAC-IN-57 elicits apoptosis in MGC-803 and HCT-116 cells in a dose-dependent manner. It also exerts inhibitory effects on LSD1 and HDACs within the MGC-803 and HCT-116 cell lines. Moreover, HDAC-IN-57 induces cell cycle arrest in the G2/M phase for both MGC-803 and HCT-116 cells.[1] HDAC-IN-57 has high metabolic stability in vitro. Retains 86.1% and 87.4% of the parent compound after 1 hour of incubation in human liver (HLM) and rat liver microsomes (RLM), respectively, with a T1/2 of over 120 minutes.[1] |
体内活性 |
HDAC-IN-57 (Compound 5e) (1 mg/kg, i.v.; 10 mg/kg, p.o.) demonstrated T1/2 of 0.37 hours (IV) and 2.75 hours (OR), with an oral bioavailability (F%) of 10.6%.[1] HDAC-IN-57 (25 or 50 mg/kg gavage; once daily for 21 days) achieved dose-dependent tumor growth inhibition in the NOD-SCID mouse MGC-803 xenograft model.[1] |
分子量 | 377.39 |
分子式 | C21H19N3O4 |
CAS No. | 2716217-79-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
HDAC-IN-57 2716217-79-5 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair HDAC HDACIN57 Inhibitor inhibitor inhibit