Almonertinib mesylate (Synonyms: HS-10296 mesylate) |
| Catalog No.GC64398 |
알모네르티닙(HS-10296) 메실레이트는 EGFR 민감성 및 T790M 내성 돌연변이에 대해 높은 선택성을 갖는 경구 사용 가능한 비가역적 3세대 EGFR 티로신 키나제 억제제입니다. 알모네르티닙 메실레이트는 T790M, T790M/L858R, T790M/Del19(IC50: 각각 0.37, 0.29, 0.21 nM)에 대해 큰 억제 활성을 보이며, 야생형(3.39 nM)에 대해서는 덜 효과적이다. Almonertinib mesylate는 비소세포폐암 연구에 사용됩니다.
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Cas No.: 2134096-06-1
Sample solution is provided at 25 µL, 10mM.
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Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer[1][2].
HS-10296 mesylate is an orally available inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity, which canbe used to treat NSCLC[2]. Additionaly, HS-10296 mesylate could also inhibit other EGFR sensitive mutations, including G719X, del19, L858R and L861Q[3].
[1]. Yang JC, et al. Safety, Efficacy, and Pharmacokinetics of Almonertinib (HS-10296) in Pretreated Patients With EGFR-Mutated Advanced NSCLC: A Multicenter, Open-label, Phase 1 Trial [published online ahead of print, 2020 Sep 9]. J Thorac Oncol. 2020;S1556-0
[2]. Sullivan I, et al. Next-Generation EGFR Tyrosine Kinase Inhibitors for Treating EGFR-Mutant Lung Cancer beyond First Line. Front Med (Lausanne). 2017 Jan 18;3:76.
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