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。
货号:ajcx29312
CAS:N/A
分子式:C30H31F3N6O6
分子量：628.6
溶解度:DMSO: 250 mg/mL (397.71 mM)
纯度：98%
存储：Store at -20°C
库存：现货

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.