Theliatinib |
| Catalog No.GC38081 |
Le théliatinib (Xiliertinib) est un inhibiteur de l'EGFR puissant, compétitif pour l'ATP, actif par voie orale et hautement sélectif avec un Ki de 0,05 nM et une IC50 de 3 nM. Le théliatinib a une IC50 de 22 nM pour le mutant EGFR T790M/L858R. Le théliatinib montre une sélectivité > 50 fois supérieure pour l'EGFR que les autres kinases. Activité anti-tumorale.
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Cas No.: 1353644-70-8
Sample solution is provided at 25 µL, 10mM.
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Theliatinib (HMPL-309) is a potent, ATP-competitive and highly selective EGFR inhibitor, significantly inhibits phosphorylation of EGFR (p-EGFR) and its downstream targets, AKT and ERK (p-AKT and p-ERK), with anti-tumor activity. Theliatinib (HMPL-309) shows a Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively[1].
[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.
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