Theliatinib (Xiliertinib) tartrate is a potent and highly selective EGFR inhibitor, displaying ATP-competitive and orally active properties. It exhibits promising efficacy with a K_i of 0.05 nM and an IC_50 of 3 nM for EGFR, alongside a specific IC_50 of 22 nM against the EGFR T790M/L858R mutant. Notably, Theliatinib demonstrates over 50-fold selectivity for EGFR compared to other kinases, underscoring its targeted action in inhibiting EGFR.

Theliatinib, a potent and highly selective EGFR inhibitor, with anti-tumor activity. Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively.