EGFR-IN-8 是 EGFR 和 c-Met 的双重抑制剂。 EGFR-IN-8可用于靶向EGFR TKI耐药的NSCLC的研究。

EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC. EGFR-IN-8 is a dual EGFR and c-Met inhibitor.

In A549, PC9, H1975, CL68, and CL97 cells, EGFR-IN-8 (0-0.6 μM; 48 hours) suppresses the expression of EGFR and c-Met in these five cell lines irrespective of their mutational status. EGFR-IN-8 (0-20 μM; 24, 48, 72 hours) exhibits a time- and dose-dependent inhibitory effect on the viability of A549, PC9, H1975, CL68, and CL97 cells at different time intervals, with IC50 values ranging from 0.3 to 0.6 μM and 0.2-0.5 μM after 48 and 72 h of treatment respectively[1].

EGFR-IN-8 (50,150 mg/kg; oral gavage) exhibits suppression (29% and 60%, respectively) of H1975 xenograft tumor growth in a dose-dependent manner[1].

2407957-87-1

C32H23ClF3N7O4

662.02

DMSO:8 mg/mL (12.08 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years