Almonertinib mesylate(Synonyms: HS-10296 mesylate)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Almonertinib mesylate (Synonyms: HS-10296 mesylate)

Almonertinib (HS-10296) mesylate 是一种口服、不可逆的第三代 EGFR 酪氨酸激酶抑制剂，对 EGFR 致敏和 T790M 耐药突变具有高选择性。Almonertinib mesylate 对 T790M、T790M/L858R 和 T790M/Del19 表现出较强的抑制活性 (IC50 分别为 0.37、0.29 和 0.21 nM)，对野生型的抑制作用较弱 (3.39 nM)。Almonertinib mesylate 用于非小细胞肺癌的研究。

Almonertinib mesylate(Synonyms: HS-10296 mesylate)

Almonertinib mesylate Chemical Structure

CAS No. : 2134096-06-1

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Almonertinib mesylate 的其他形式现货产品:

Almonertinib Almonertinib hydrochloride

生物活性

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].

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

621.75

Formula

C31H39N7O5S
CAS 号

2134096-06-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vitro: 

DMSO : 31.25 mg/mL (50.26 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6084 mL 8.0418 mL 16.0836 mL
5 mM 0.3217 mL 1.6084 mL 3.2167 mL
10 mM 0.1608 mL 0.8042 mL 1.6084 mL

参考文献

  • [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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