Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lazertinib (GNS-1480) 是一种高度突变选择性和不可逆的 EGFR-TKI,可用于非小细胞肺癌的研究,对 Del19/T790M、L858R/T790M、Del19、L85R 和野生型 EGFR 的 IC50 值分别为 1.7、2、5、20.6 和 76 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 328 | 现货 | ||
2 mg | ¥ 476 | 现货 | ||
5 mg | ¥ 788 | 现货 | ||
10 mg | ¥ 1,160 | 现货 | ||
25 mg | ¥ 2,160 | 现货 | ||
50 mg | ¥ 3,490 | 现货 | ||
100 mg | ¥ 5,120 | 现货 | ||
500 mg | ¥ 10,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 962 | 现货 |
产品描述 | Lazertinib (GNS-1480) is an effective, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively. |
靶点活性 | Del19:5 nM, Del19/T790M:1.7 nM, L85R:20.6 nM, EGFR (WT):76 nM, EGFR (L858R/T790M):2 nM |
体外活性 | In NSCLC cell lines and primary cancer cells from patients harbouring EGFR mutations, YH25448 more potently inhibits cancer cell growth and significantly increases tumour cell apoptosis compared to osimertinib[1]. In the cell proliferation assays, GI50 values of Lazertinib are 6 nM, 5 nM, and 711 nM for H1975 cells (L858R/T790M), PC9 cells (del19) and H2073 cells (wt), respectively. |
体内活性 | In an in vivo mouse model implanted with H1975 cells, once-daily YH25448 treatment results in dramatic dose-dependent tumour regression in both subcutaneous and intracranial lesions with no abnormal signs such as skin keratosis. The plasma half-life of YH25448 is 5.9-6.8 hr, while a tumour to plasma AUC0-last ratio is 3.0-5.1 in tumour-bearing mice. YH25448 shows excellent penetration of the blood-brain barrier, achieving CSF concentrations exceeding the IC50 value for pEGFR inhibition. YH25448 shows superior efficacy for tumour regression in an EGFR mutant brain metastasis model[1]. |
细胞实验 | Concentrations: 5, 10, 100 nM. Ba/F3 cells overexpressing the indicated EGFR mutant are treated with YH25448 or osimertinib for 6 hours at the indicated concentrations. pEGFR levels are detected by Western blot analysis. |
别名 | Lazertinib (YH25448), GNS-1480, YH25448 |
分子量 | 554.64 |
分子式 | C30H34N8O3 |
CAS No. | 1903008-80-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5.55 mg/mL (10 mM), Sonication is recommended.
Ethanol: Insoluble
H2O: Insoluble
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.803 mL | 9.0149 mL | 18.0297 mL | 45.0743 mL |
5 mM | 0.3606 mL | 1.803 mL | 3.6059 mL | 9.0149 mL | |
10 mM | 0.1803 mL | 0.9015 mL | 1.803 mL | 4.5074 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。
Lazertinib 1903008-80-9 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Lazertinib (YH25448) ErbB-1 GNS1480 GNS-1480 Inhibitor Epidermal growth factor receptor HER1 YH 25448 YH-25448 GNS 1480 YH25448 inhibit inhibitor