EGFR-IN-1 TFA

EGFR-IN-1TFA是一种口服活性不可逆的突变型选择性L858R/T790MEGFR抑制剂。与野生型EGFR相比，EGFR-IN-1TFA对Gefitinib耐药的EGFRL858R/T790M有100倍的抑制作用。EGFR-IN-1TFA对H1975细胞和HCC827细胞具有较强的抗增殖活性。具有抗肿瘤活性。

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
5mg

￥5175.00

4140.00

- +
10mg

￥8637.00

6910.00

- +
25mg

￥18162.00

14530.00

- +
50mg

￥29925.00

23940.00

- +
100mg

￥45950.00

36760.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

Background

EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity[1].

EGFR-IN-1 TFA (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity[1]. Cell Proliferation Assay[1] Cell Line: NSCLC cell lines H1975 (T790M/L858R), HCC827 (?746-750)

EGFR-IN-1 TFA (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight[1].EGFR-IN-1 TFA evaluates in a time course PD experiment upon oral dosing at 30 mg/kg. EGFR-IN-1 TFA shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 TFA reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h[1].

[1]. Wurz RP, et al. Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. ACS Med Chem Lett. 2015 Jul 27;6(9):987-92.