Almonertinib mesylate (Synonyms: HS-10296 mesylate) |
| カタログ番号GC64398 |
アルモネルチニブ (HS-10296) メシル酸塩は、EGFR 感作変異および T790M 耐性変異に対して高い選択性を持つ、経口投与可能な不可逆的な第 3 世代の EGFR チロシンキナーゼ阻害剤です。メシル酸アルモネルチニブは、T790M、T790M/L858R、および T790M/Del19 に対して優れた阻害活性を示し (IC50: それぞれ 0.37、0.29、および 0.21 nM)、野生型に対してはあまり効果がありません (3.39 nM)。メシル酸アルモネルチニブは、非小細胞肺がんの研究に使用されています。
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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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