DHFR-IN-4 is a potent didrofolate reductase (DHFR) inhibitor with an IC50 value of 123 nM. DHFR-IN-4 also has inhibitory activity against EGFR and HER2 with IC50s of 246 nM and 357 nM, respectively. DHFR-IN-4 has remarkable broad spectrum cytotoxic potency against cancer cells.
DHFR-IN-4 (compound 42) (0-100 μM; 72 h) shows remarkable broad spectrum cytotoxic potency against HepG2, MCF-7, HCT-116, PC3 and HeLa[1].
References:
[1]. Sabry MA, et al. New thiazole-based derivatives as EGFR/HER2 and DHFR inhibitors: Synthesis, molecular modeling simulations and anticancer activity. Eur J Med Chem. 2022 Aug 10;241:114661.