Theliatinib

Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a K_i of 0.05 nM and an IC₅₀ of 3 nM. Theliatinib has an IC₅₀ of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases^[1]. Theliatinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. IC50 & Target:IC50: 3 nM (EGFR), 22 nM (EGFR T790M/L858R)^[1]
Ki: 0.05 nM (EGFR)^[1] In Vitro:Theliatinib significantly inhibits EGFR phosphorylation in A431 cells with an IC₅₀ of 7 nM. Theliatinib also inhibits A431, H292 and FaDu cells survival with IC₅₀ values of 80 nM, 58 nM and 354 nM, respectively^[1]. In Vivo:Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of 75% at the end of study, and with a dose response^[1].