Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Nazartinib mesylate is a novel, covalent mutant-selective inhibitor of EGFR (Ki and Kinact: 31 nM and 0.222/min on EGFR(L858R/790M) mutant).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
Nazartinib mesylate 的其他形式现货产品:
产品描述 | Nazartinib mesylate is a novel, covalent mutant-selective inhibitor of EGFR (Ki and Kinact: 31 nM and 0.222/min on EGFR(L858R/790M) mutant). |
靶点活性 | EGFR (L858R/T790M):31 nM (ki) |
体外活性 | Nazartinib inhibits cell proliferation (EC50: 9, 11, and 25 nM in H3255, HCC827, and H1975, respectively). Nazartinib has an inhibitory effect on the mutant cell lines (IC50s: 4, 6, 2 nM in H1975, H3255, and HCC827, respectively). It also shows improved ADME and PK properties [1]. Nazartinib has an OC50 value of 2 and 5 nM on HCC827 and H1975, respectively. Nazartinib displays potent inhibition of pEGFR levels in H3255, HCC827, and H1975 cell lines ( EC50: 5, 1, and 3 nM, respectively) [2]. |
体内活性 | Nazartinib (50 and 20 mg/kg or 25 mg/kg, p.o.) demonstrates dose-dependent efficacy with near-complete tumor cells regression at the highest dose tested (50 mg/kg), in H1975 mouse xenograft model [1]. Nazartinib (30 mg/kg, p.o.) displays significant antitumor activity, in the H3255 xenograft model. In the H1975 mouse model, Nazartinib (10 mg/kg, p.o.) induces tumor growth inhibition with a T/C (tumor/control volume) of 29%, and when doses are 30 and 100 mg/kg, tumor regressions are achieved (T/C, ?61% and ?80%, respectively). Antiproliferative activity of Nazartinib on 89 lung cancer cell lines indicates that Nazartinib selectively inhibits cell lines containing EGFR with catalytic domain mutations [2]. |
别名 | EGF816 (mesylate) |
分子量 | 591.12 |
分子式 | C27H35ClN6O5S |
CAS No. | 1508250-72-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
Nazartinib mesylate 1508250-72-3 Others EGF 816 EGF816 (mesylate) EGF-816 EGF816 Nazartinib Mesylate Inhibitor inhibitor inhibit