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, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Theliatinib 顯著抑制 A431 細(xì)胞中的 EGFR 磷酸化，IC₅₀ 為 7 nM。Theliatinib 還抑制 A431、H292 和 FaDu 細(xì)胞存活，IC₅₀ 值分別為 80 nM、58 nM 和 354 nM^[1]。

MCE 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

442.51

C₂₅H₂₆N₆O₂

1353644-70-8

固體

White to off-white

西利替尼

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]