Powder: -20°C for 3 years | In solvent: -80°C for 1 year
WZ8040 是一种新型突变选择性不可逆 EGFRT790M 抑制剂,可抑制EGFR 磷酸化。它对突变型EGFR 的活性是野生型EGFR 的100倍以上。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 397 | 现货 | ||
5 mg | ¥ 978 | 现货 | ||
10 mg | ¥ 1,560 | 现货 | ||
25 mg | ¥ 2,570 | 现货 | ||
50 mg | ¥ 3,860 | 现货 | ||
100 mg | ¥ 5,520 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,070 | 现货 |
产品描述 | WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I). |
靶点活性 | HCC827 (EGFR Del E746_A750):1 nM, H1819 (ERBB2 amp):738 nM , PC9 GR (EGFR Del E746_A750/T790M):8 nM, PC9 (EGFR Del E746_A750):6 nM, H1781 (ERBB2 Ins G776V, C):744 nM , HCC827 GR (EGFR E746_A750/MET amp):>3.3 μM, H1975 (EGFR L858R/T790M):9 nM, H3255 (EGFR L858R):66 nM, Calu-3 (ERBB2 amp):915 nM |
体外活性 | WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ8040 treatment potently inhibits the growth of HCC827 (EGFR Del E746_A750), PC9 (EGFR Del E746_A750), H3255 (EGFR L858R), H1975 (EGFR L858R/T790M), and PC9 GR (EGFR Del E746_A750/T790M) with IC50 of 1 nM, 6 nM, 66 nM, 9 nM, and 8 nM, respectively. WZ8040 weakly inhibits the growth of HCC827 GR (EGFR E746_A750/MET amp), H1819 (ERBB2 amp), Calu-3 (ERBB2 amp), H1781 (ERBB2 Ins G776V, C), and HN11 (EGFR & ERBB2 WT) with IC50 of >3.3 μM, 738 nM, 915 nM, 744 nM, and 1.82 μM, respectively. WZ8040 is not toxic up to 10 μM against A549 (KRAS mutant) or H3122 (EML4-ALK) cells. [1] |
细胞实验 | Cells are exposed to increasing concentrations of WZ8040 for 72 hours. Growth is assessed using the MTS survival assay.(Only for Reference) |
分子量 | 481.01 |
分子式 | C24H25ClN6OS |
CAS No. | 1214265-57-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 3 mg/mL (6.23 mM)
DMSO: 89 mg/mL (185 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.079 mL | 10.3948 mL | 20.7896 mL | 51.974 mL |
5 mM | 0.4158 mL | 2.079 mL | 4.1579 mL | 10.3948 mL | |
DMSO | 10 mM | 0.2079 mL | 1.0395 mL | 2.079 mL | 5.1974 mL |
20 mM | 0.1039 mL | 0.5197 mL | 1.0395 mL | 2.5987 mL | |
50 mM | 0.0416 mL | 0.2079 mL | 0.4158 mL | 1.0395 mL | |
100 mM | 0.0208 mL | 0.1039 mL | 0.2079 mL | 0.5197 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。
WZ8040 1214265-57-2 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR HER1 mutated Inhibitor phosphorylation WZ 8040 NSCLC Epidermal growth factor receptor inhibit WZ-8040 ErbB-1 inhibitor