Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Zorifertinib (AZD3759) 是一种可口服的中枢神经系统渗透性 EGFR 抑制剂,对 EGFRwt、EGFRL858R 和 EGFRexon 19Del,IC50分别为 0.3、0.2 和 0.2 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 289 | 现货 | ||
25 mg | ¥ 439 | 现货 | ||
50 mg | ¥ 578 | 现货 | ||
100 mg | ¥ 912 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 316 | 现货 |
产品描述 | Zorifertinib (AZD3759) is an orally active, effective and central nervous system-penetrant EGFR inhibitor. The IC50 values were 0.2, 0.3 and 0.2 nM for EGFR L858R mutant, TK wild-type, and Exon 19Del enzymes, respectively. |
靶点活性 | TK (WT):0.3nM, EGFR (exon 19 deletion):0.2 nM, EGFR (L858R):0.2nM |
体外活性 | In H3255 (L858R) cells, AZD3759 inhibits EGFR phosphorylation with IC50 of 7.2 nM. AZD3759 demonstrates inhibitory effects on both the pEGFR pathway and cell proliferation of EGFR mutation-derived cells PC-9 and H3255 with IC50 of 7.7 nM and 7 nM, respectively, showing mo activity on cell proliferation of H838 cells. [1] |
体内活性 | AZD3759 shows good oral bioavailability in dogs, and penetrates extensively into monkey brain. In a brain metastasis PC-9 (Exon19Del) model, AZD3759 (15 mg/kg) causes significant dose-dependent antitumor efficacy. [1] |
激酶实验 | IC50 determination of compounds against EGFR enzymes: The inhibition potency of compounds against EGFR WT and mutant enzymes is assessed using CisBio homogenous time resolved fluorescence approach (HTRF, Cat No. 62TK0PEJ) according to manufacturer's instruction. The final enzyme concentrations used in this assay are 0.1 nM, 0.03 nM, and 0.026 nM for EGFR wild type, L858R and Exon19Del, respectively, and 0.8 μM, 4 μM and 25 μM ATP, corresponding to the Km values of EGFR enzymes, are applied accordingly. In brief, 3 μL of ATP and 2 μM TK biotin-peptide substrate are incubated in the presence or absence of serially diluted compound at room temperature in 384-well Greiner white polystyrene assay plates. The reaction is initiated by addition of 3 μL kinase which could phosphorylate the substrate peptide, and the assay buffer contains 1 mM DTT, 5 mM MgCl2, 1 mM MnCl2, and 0.01% CHAPS. After 30 minutes incubation, the reaction is stopped by the addition of 6 μl detection reagent mix containing 250 nM Strep-XL665 and TK Ab Europium Cryptate diluted in detection buffer. The plates are incubated for 1 h before the fluorescence is then measured at 615 nm and 665 nm, respectively with excitation wavelength at 320 nm by EnVision Multilabel Reader from Perkin Elmer using standard HTRF settings. The calculated signal ratio of 665 nm/615 nm is proportional to the kinase activity. The concentration of compound producing 50% inhibition of the respective kinase (IC50) is calculated using four-parameter logistic fit. |
细胞实验 | Cell proliferation assay is determined by MTS methods. Briefly, cells are seeded in 96-well plates (at a density to allow for logarithmic growth during the 72-hour assay) and incubated overnight at 37 °C and 5% CO2. Cells are then exposed to concentrations of compounds ranging from 30 to 0.0003 mM for 72 hours. For the MTS endpoint, cell proliferation is measured by the CellTiter AQueous Non-Radioactive Cell Proliferation Assay reagent in accordance with the manufacturer's protocol. Absorbance is measured with a Tecan Ultra instrument. Predose measurements are made, and concentration needed to reduce the growth of treated cells to half that of untreated cells (GI50) values are determined using absorbance readings.(Only for Reference) |
别名 | AZD3759 |
分子量 | 459.9 |
分子式 | C22H23ClFN5O3 |
CAS No. | 1626387-80-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 50 mg/mL (108.72 mM)
Ethanol: 18 mg/mL(39.1 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.1744 mL | 10.8719 mL | 21.7439 mL | 54.3596 mL |
5 mM | 0.4349 mL | 2.1744 mL | 4.3488 mL | 10.8719 mL | |
10 mM | 0.2174 mL | 1.0872 mL | 2.1744 mL | 5.436 mL | |
20 mM | 0.1087 mL | 0.5436 mL | 1.0872 mL | 2.718 mL | |
DMSO | 50 mM | 0.0435 mL | 0.2174 mL | 0.4349 mL | 1.0872 mL |
100 mM | 0.0217 mL | 0.1087 mL | 0.2174 mL | 0.5436 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。
Zorifertinib 1626387-80-1 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR AZD-3759 inhibit AZD3759 ErbB-1 HER1 Inhibitor Epidermal growth factor receptor AZD 3759 inhibitor