Powder: -20°C for 3 years | In solvent: -80°C for 1 year
WZ3146是一种突变选择性EGFR 抑制剂,对EGFRL858R、EGFRL858R/T790M、EGFRE746_A750、EGFRE746_A750/T790M 和 EGFR 的IC50值分别为2、2、5、14 和 66 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 397 | 现货 | ||
2 mg | ¥ 595 | 现货 | ||
5 mg | ¥ 995 | 现货 | ||
10 mg | ¥ 1,760 | 现货 | ||
25 mg | ¥ 3,180 | 现货 | ||
50 mg | ¥ 4,660 | 现货 | ||
100 mg | ¥ 6,630 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,080 | 现货 |
产品描述 | WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I). |
靶点活性 | EGFR (L858R):2 nM |
体外活性 | WZ3146 significantly suppresses the growth of EGFR mutation containing cell lines with IC50 of 3 nM in EGFR Del E746_A750 containing HCC827 cells, 15 nM in EGFR Del E746_A750 containing PC9 cells, 29 nM in EGFR L858R/T790M containing H1975 cells and 3 nM in EGFR Del E746_A750/T790M containing PC9 GR cells. [1] |
激酶实验 | In-vitro inhibitory enzyme kinetic assays: The assays are carried out in triplicate using the ATP/NADH coupled assay system in a 96-well format. The final reaction mixture contains 0.5 mg/mL Bovine Serum Albumin (BSA), 2 mM MnCl2, 1 mM phospho(enol) pyruvic acid (PEP), 1 mM TCEP, 0.1 M Hepes 7.4, 2.5 mM poly-[Glu4Tyr1] peptide, 1/50 of the final reaction mixture volume of pyruvate kinase/lactic dehydrogenase enzymes from rabbit muscle, 0.5 mM NADH, 0.5 μM EGFR kinase, 100 μM ATP and varied amount of WZ3146. WZ3146 and ATP are mixed and made separate stock from the mixture with all other ingredients and added last to the latter to start the reaction. Steady state initial velocity data are drawn from the slopes of the A340 curves. |
细胞实验 | Growth and inhibition of growth is assessed by MTS assay. NSCLC or Ba/F3 cells are exposed to treatment for 72 hours and the number of cells used per experiment is determined empirically. All experimental points are set up in six to twelve wells and all experiments are repeated at least three times. The data is graphically displayed using GraphPad Prism version 5.0 for Windows. The curves are fitted using a non-linear regression model with a sigmoidal dose response.(Only for Reference) |
分子量 | 464.95 |
分子式 | C24H25ClN6O2 |
CAS No. | 1214265-56-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 86 mg/mL (185 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
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 | 2.1508 mL | 10.7538 mL | 21.5077 mL | 53.7692 mL |
5 mM | 0.4302 mL | 2.1508 mL | 4.3015 mL | 10.7538 mL | |
10 mM | 0.2151 mL | 1.0754 mL | 2.1508 mL | 5.3769 mL | |
20 mM | 0.1075 mL | 0.5377 mL | 1.0754 mL | 2.6885 mL | |
50 mM | 0.043 mL | 0.2151 mL | 0.4302 mL | 1.0754 mL | |
100 mM | 0.0215 mL | 0.1075 mL | 0.2151 mL | 0.5377 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。
WZ-3146 1214265-56-1 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR HER1 Epidermal growth factor receptor WZ3146 WZ 3146 ErbB-1 inhibit Inhibitor inhibitor