Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AES-350 是一种具有口服活性HDAC6抑制剂,IC50和Ki 分别为 0.0244 μM 和 0.035 μM。它对 HDAC3、8 和 11 的 IC50值分别为 0.187、0.245和大于1μM。它通过抑制 HDAC 诱导 AML 细胞凋亡,可研究急性髓系白血病。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,160 | 现货 | ||
5 mg | ¥ 2,790 | 现货 | ||
10 mg | ¥ 4,150 | 现货 | ||
25 mg | ¥ 6,630 | 现货 | ||
50 mg | ¥ 8,850 | 现货 | ||
100 mg | ¥ 11,900 | 现货 | ||
500 mg | ¥ 24,300 | 现货 |
产品描述 | AES-350 is a potent and orally active HDAC6 inhibitor(IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively). It is also against HDAC-3, -8, and -11 in an enzymatic activity assay with IC50 values of 0.187 μM, 0.245 μM, and >1μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research. |
靶点活性 | HDAC6:24.4 nM, HDAC11:245 nM , HDAC3:187 nM |
体外活性 | AES-350 (0.25-4 μM;?18 hours) induces MV4-11 cells apoptosis in a dose-dependent manner.?The late apoptosis ratios are 8.74%, 11.7%,16.08%, 30.97%, and 38.48%, respectively at 0.25 μM-4 μM.?AES-350 has submicromolar activity (IC50=0.58±0.13 μM) against MV4-11 cells than to that of vorinostat (IC50=0.31±0.061 μM).?AES-350 is more ligand efficient and exemplifies a large therapeutic index (IC50>30 μM in noncancerous MRC-9 cells).?AES-350 is also shown to be effective in AML-3 (acute myeloid leukemia) cells (IC50=0.73 ± 0.12 μM).?An ELISA is performed using HeLa cervical cancer cell lysates, and HeLa cells highly express HDAC6 and are sensitive to AES-350.?Correspondingly, ELISA assays depicted a dose-dependent increase in HDAC6 inhibition (IC50=0.58±0.13 μM), Western blot analysis shows that AES-350 (0.1-10 μM) induces a dose-dependent increase in acetylated α-tubulin (Ac-α-tubulin), a substrate of HDAC. |
分子量 | 312.36 |
分子式 | C18H20N2O3 |
CAS No. | 847249-57-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (320.14 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 | 3.2014 mL | 16.0072 mL | 32.0143 mL | 80.0359 mL |
5 mM | 0.6403 mL | 3.2014 mL | 6.4029 mL | 16.0072 mL | |
10 mM | 0.3201 mL | 1.6007 mL | 3.2014 mL | 8.0036 mL | |
20 mM | 0.1601 mL | 0.8004 mL | 1.6007 mL | 4.0018 mL | |
50 mM | 0.064 mL | 0.3201 mL | 0.6403 mL | 1.6007 mL | |
100 mM | 0.032 mL | 0.1601 mL | 0.3201 mL | 0.8004 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。
AES-350 847249-57-4 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Histone deacetylases MV4-11 acute myeloid leukemia AML Inhibitor AES 350 inhibit AES350 inhibitor