Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD1208 是一种具有口服活性的高度选择性PIM 抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 268 | 现货 | ||
5 mg | ¥ 492 | 现货 | ||
10 mg | ¥ 713 | 现货 | ||
25 mg | ¥ 1,370 | 现货 | ||
50 mg | ¥ 2,480 | 现货 | ||
100 mg | ¥ 3,720 | 现货 | ||
200 mg | ¥ 5,230 | 现货 | ||
500 mg | ¥ 7,920 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 507 | 现货 |
产品描述 | AZD1208 is a novel, orally bioavailable, highly selective PIM kinase inhibitor with single nanomolar potency against all three PIM kinases. |
靶点活性 | Pim2:5 nM, Pim3:1.9 nM, Pim1:0.4 nM |
体外活性 | AZD1208剂量依赖性抑制MOLM-16和KG-1a异种移植肿瘤在体内的生长. |
体内活性 | AZD1208在培养的MOLM-16细胞中引起细胞周期停滞和细胞凋亡。 这伴随着BAD,4EBP1和p70S6K磷酸化的剂量依赖性降低。 另外,AZD1208导致有效抑制来自骨髓抽吸物的原代AML细胞的集落生长并下调Pim靶标的磷酸化。 |
激酶实验 | The activity of purified human PIM-1, PIM-2 and PIM-3 enzymes on substrate FL-Ahx-Bad (FITC-(AHX)RSRHSSYPAGT-COOH) is determined using a mobility shift assay on a Caliper LC3000 reader. The PIM-1 assay is performed in a 12 mL reaction containing 50 mM HEPES (pH 7.5), 1 mM DTT, 0.01% Tween 20, 50 mg/mL BSA, 10 mM MgCl2, 1.5 mM FL-Ahx-Bad peptide, 100 mM ATP, 2.5 nM PIM-1 and various amount of inhibitor. The reaction is quenched after 90 minute incubation at 25?C with?5 mL of stop mix consisting of 100 mM HEPES, 121 mM EDTA, 0.8% Coating Reagent 3 and 0.01% Tween 20. The ATP and enzyme concentrations for the PIM-2 assay are 5 mM and 2.5 nM, respectively, while 50 mM of ATP and 0.33 nM of enzyme is used for PIM-3 assays. For high [ATP] screenings, 5 mM ATP is used with 0.67 nM enzyme for both PIM-1 and PIM-2 or 0.11 nM PIM-3. Fluorescence of phosphorylated and unphosphorylated substrate is detected and a ratiometric value is calculated to determine percent turnover. IC50 values are determined from dose-response data using IDBS ActivityBase software. |
细胞实验 | AZD1208 is dissolved in DMSO. MOLM-16 cells, purchased from DSMZ and cultured in RPMI containing 10% fetal bovine serum (FBS) and 1% L-glutamine, are plated at 20,000 cells per well in 96 well plates overnight. Cells are treated for 72 hours with compound or control vehicle (dimethyl sulfoxide) and cell viability is measured after the addition of Cell Titer-Blue for 4 hours at 37?C and reading of fluorescence on a Tecan Infinite? 200. The GI50 is determined by calculating growth at each dose relative to vehicle treated cells and cell viability at the time of treatment. |
分子量 | 379.48 |
分子式 | C21H21N3O2S |
CAS No. | 1204144-28-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 7.6 mg/mL (20 mM), with gentle warming
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6352 mL | 13.1759 mL | 26.3518 mL | 65.8796 mL |
5 mM | 0.527 mL | 2.6352 mL | 5.2704 mL | 13.1759 mL | |
10 mM | 0.2635 mL | 1.3176 mL | 2.6352 mL | 6.588 mL | |
20 mM | 0.1318 mL | 0.6588 mL | 1.3176 mL | 3.294 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。
AZD1208 1204144-28-4 Apoptosis Autophagy Chromatin/Epigenetic JAK/STAT signaling Pim inhibit AZD-1208 Pim kinases Inhibitor AZD 1208 inhibitor