| 名称 | Lazertinib |
| 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. |
| 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. |
| 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 Lazertinib 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 Lazertinib is 5.9-6.8 hr, while a tumour to plasma AUC0-last ratio is 3.0-5.1 in tumour-bearing mice. Lazertinib shows excellent penetration of the blood-brain barrier, achieving CSF concentrations exceeding the IC50 value for pEGFR inhibition. Lazertinib shows superior efficacy for tumour regression in an EGFR mutant brain metastasis model[1]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 5.55 mg/mL (10 mM), Sonication is recommended.
Ethanol : Insoluble
H2O : Insoluble
|
| 关键字 | ErbB-1 | GNS1480 | EGFR | Inhibitor | Epidermal growth factor receptor | HER1 | YH 25448 | YH-25448 | GNS 1480 | inhibit | Lazertinib |
| 相关产品 | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Afatinib Dimaleate | Erlotinib hydrochloride | Erlotinib | Neratinib | Chalcone | Osimertinib mesylate | Genistein | Khellin | Gefitinib |
| 相关库 | 高选择性抑制剂库 | 经典已知活性库 | 膜蛋白靶向化合物库 | 酪氨酸激酶分子库 | 激酶抑制剂库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 已知活性化合物库 | 抗癌药物库 | 抗癌活性化合物库 |
United States
