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CAS No.: 1903008-80-9

Lazertinib Catalog No. CSN21195

Synonyms: YH25448;GNS-1480

Lazertinib is a selective inhibitor of mutant EGFR with lowest activity against EGFR wild type.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Lazertinib is the third-generation, highly mutant-selective, irreversible and brain permeable EGFR inhibitor with IC50 values of 2 nM and 76 nM for EGFR^L858R/T790M and WT EGFR, respectively. Lazertinib exhibited more potency of anti-proliferative effect on NSCLC cell lines and primary cancer cells from patients harboring EGFR mutations, shown as GI50 values were 6 nM, 5 nM, and 711 nM for H1975 cells (L858R/T790M), PC9 cells (del19) and H2073 cells (wt), respectively, and significantly increased tumor cell apoptosis compared to osimertinib. Once-daily treatment subcutaneously or intracranially with lazertinib at dose ranging in 1-25 mg/kg showed a dramatic dose-dependent tumor regression in mouse model implanted with H1975 cells, without abnormal signs such as skin keratosis shown in osimertinib-treated mice. Specially, lazertinib showed excellent penetration of the blood-brain barrier, achieving CSF concentrations exceeding the IC50 value for pEGFR inhibition in the tumor-bearing mice^[1]^[2].

动物研究

剂量

Mice^[3] (p.o.): 1 mg/kg - 10 mg/kg

给药途径

p.o.

动物药代数据

Animal	Nude mice^[3]
Dose	10 mg/kg
Administration	p.o.
AUC_{last(intracranial tumor/brain)}	7.9
T_max	4 h
AUC_{last(intracranial tumor/plasma)}	7

参考文献

[1] Jiyeon Y, Min HH, et al. YH25448, an irreversible 3rd generation EGFR TKI, exhibits superior anticancer effects with potent brain BBB penetration in NSCLC. Abstract 4790, Cancer Research, Volume 78, Issue 13 Supplement, pp. 4790.
[2] Min H H, In Y L, et al. P3.02b-119 YH25448, a Highly Selective 3rd Generation EGFR TKI, Exhibits Superior Survival over Osimertinib in Animal Model with Brain Metastases from NSCLC. JTO, Volume 12, Issue 1, Supplement, Pages S1265–S1266.
[3] Yun J, Hong MH, et al. YH25448, an Irreversible EGFR-TKI with Potent Intracranial Activity in EGFR Mutant Non-Small Cell Lung Cancer. Clin Cancer Res. 2019 Apr 15;25(8):2575-2587.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8030 mL
- 9.0148 mL
- 18.0296 mL
- 5 mM
- 0.3606 mL
- 1.8030 mL
- 3.6059 mL
- 10 mM
- 0.1803 mL
- 0.9015 mL
- 1.8030 mL

技术信息

CAS号

1903008-80-9

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H34N8O3

运输

蓝冰

分子量

554.64

别名

YH25448;GNS-1480

溶解度

DMSO	4.0 mg/mL (7.2 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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