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 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].

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

Theliatinib tartrate (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].

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

592.60

C₂₉H₃₂N₆O₈

2413487-72-4

O=C(N1C[C@]2([H])N(C)CC[C@]2([H])C1)NC3=CC4=C(NC5=CC=CC(C#C)=C5)N=CN=C4C=C3OC.OC([C@H](O)[C@@H](O)C(O)=O)=O

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]