Theliatinib |
| Catalog No.GC38081 |
Theliatinib (Xiliertinib) es un inhibidor de EGFR potente, competitivo con ATP, activo por vÍa oral y altamente selectivo con una Ki de 0,05 nM y una IC50 de 3 nM. Theliatinib tiene una IC50 de 22 nM para el mutante EGFR T790M/L858R. Theliatinib muestra una selectividad >50 veces mayor por EGFR que otras quinasas. Actividad antitumoral.
Products are for research use only. Not for human use. We do not sell to patients.
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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