Theliatinib |
| カタログ番号GC38081 |
テリアチニブ (Xiliertinib) は、0.05 nM の Ki と 3 nM の IC50 を持つ、強力で、ATP 競合的で、経口活性があり、選択性の高い EGFR 阻害剤です。テリアチニブの EGFR T790M/L858R 変異体に対する IC50 は 22 nM です。テリアチニブは、EGFR に対して他のキナーゼよりも 50 倍以上の選択性を示します。抗腫瘍活性。
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.
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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