aladdin 阿拉丁 L414136 Lazertinib 1903008-80-9 98%

中文名：Lazertinib

英文名：Lazertinib

纯度：Moligand™，≥98%

货号：L414136

Cas号：1903008-80-9

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversibleEGFR-TKIwith 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, showing much higher IC50 values aganist ErbB2 and ErbB4.

Targets

Del19/T790M (Cell-free assay); L858R/T790M EGFR (Cell-free assay); Del19 (Cell-free assay); L85R (Cell-free assay); WT EGFR (Cell-free assay) 1.7 nM; 2 nM; 5 nM; 20.6 nM; 76 nM

In vitro

Lazertinib targets the activating EGFR mutations Del19 and L858R, as well as the T790M mutation, while sparing wild type. In NSCLC cell lines and primary cancer cells from patients harboring EGFR mutations, YH25448 more potently inhibits cancer cell growth and significantly increases tumor cell apoptosis compared to osimertinib. 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.

In vivo

In an in vivo mouse model implanted with H1975 cells, once-daily YH25448 treatment results in indramatic dose-dependent tumor 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 the tumor to plasma AUC_0-last ratio is 3.0-5.1 in tumor-bearing mice. YH25448 shows excellent penetration of the blood-brain bartier, achieving CSF concentrations exceeding the IC50 value for pEGFR inhibition. YH25448 shows superior efficacy for tumor regression in an EGFR mutant brain metastasis model.

Cell Research(from reference)

Cell lines：Ba/F3 cells 

Concentrations：5, 10, 100 nM 

Incubation Time：6 h 

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