Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EHT 1610 (EHT 5372) 是双特异性酪氨酸磷酸化调节酶 (DYRK) 的强效抑制剂,对 DYRK1A 和 DYRK1B 有抑制作用,的 IC50 分别为 0.36 nM 和 0.59 nM。EHT 1610 对白血病具有抑制效应,可调节细胞周期,诱导细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,470 | 现货 | ||
5 mg | ¥ 3,590 | 现货 | ||
10 mg | ¥ 5,190 | 现货 | ||
25 mg | ¥ 7,920 | 现货 | ||
50 mg | ¥ 10,900 | 现货 | ||
100 mg | ¥ 14,600 | 现货 | ||
500 mg | ¥ 29,300 | 现货 |
产品描述 | EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis. |
靶点活性 | DYRK2:10.8 nM, CLK1:22.8 nM, DYRK1B:0.28 nM, DYRK1A:0.22 nM, CLK2:88.8 nM, CLK4:59 nM, GSK-3α:7.44 nM, β-glucuronidase:93.2 nM, GSK-3β:221 nM, DYRK1A:0.36 nM, DYRK1B:0.59 nM |
体外活性 |
EHT 1610 triggers apoptosis in primary ALL cells that exhibit resistance to cytarabine treatment.[2] EHT 1610 demonstrates a dose-dependent induction of apoptosis in B- and T-cell lines as well as primary human pediatric cells.[2] Treatment with EHT 1610 for a duration of 72 hours leads to the inhibition of DYRK1A, resulting in the disruption of DYRK1A-mediated FOXO1 and STAT3 signaling pathways. This disruption ultimately leads to selective cell death in leukemic B cells.[3] Exposure to EHT 1610 at concentrations ranging from 2.5 to 10 μM for a period of 4-5 hours results in the inhibition of phosphorylation of FOXO1, STAT3, and cyclin D3. This inhibition leads to the regulation of late cell-cycle progression, mitochondrial ROS levels, and DNA damage, respectively.[3] |
体内活性 | In a murine model of aggressive leukemia, EHT 1610 (20 mg/kg/d; i.p.; twice a day; 3 weeks) demonstrates antileukemia activity when administered intraperitoneally.[3] |
别名 | EHT 5372 |
分子量 | 383.4 |
分子式 | C18H14FN5O2S |
CAS No. | 1425945-60-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4.5 mg/mL (11.7 mM), Sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6082 mL | 13.0412 mL | 26.0824 mL | 65.2061 mL |
5 mM | 0.5216 mL | 2.6082 mL | 5.2165 mL | 13.0412 mL | |
10 mM | 0.2608 mL | 1.3041 mL | 2.6082 mL | 6.5206 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。
EHT 1610 1425945-60-3 Cell Cycle/Checkpoint NF-Κb PI3K/Akt/mTOR signaling Proteases/Proteasome Stem Cells Tyrosine Kinase/Adaptors GSK-3 NF-κB Tyrosinase DYRK CDK EHT5372 EHT-5372 EHT1610 EHT-1610 EHT 5372 Inhibitor inhibitor inhibit