Theliatinib tartrate  (Synonyms: Xiliertinib tartrate; HMPL-309 tartrate)

Theliatinib (Xiliertinib) tartrate 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 (tartrate) 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 tartrate 显着抑制 A431 细胞中的 EGFR 磷酸化，IC₅₀ 为 7 nM。Theliatinib 还抑制 A431、H292 和 FaDu 细胞存活，IC₅₀ 值分别为 80 nM、58 nM 和 354 nM^[1]。

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

Theliatinib tartrate（2-15 mg/kg；口服；每天；21 天；NOD-SCID 小鼠；PDECX 1T0950 模型）导致小鼠模型中的肿瘤消退 75%，并且呈剂量依赖性^[1]。

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

592.60

C₂₉H₃₂N₆O₈

2413487-72-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]