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. Anti-tumor activity^[1].

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

442.51

C₂₅H₂₆N₆O₂

1353644-70-8

西利替尼

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• [1]. Ren Y, et al. Anti-tumor efficacy of theliatinib in esophageal cancer patient-derived xenografts models with epidermal growth factor receptor (EGFR) overexpression and gene amplification. Oncotarget. 2017 Apr 19;8(31):50832-50844.