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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-Almonertinib
Almonertinib

Chemical Structure : Almonertinib

CAS No.: 1899921-05-1

Almonertinib (HS-10296, HS10296)

货号: PC-38342Not For Human Use, Lab Use Only.

Aumolertinib (HS-10296) is a novel, third-generation EGFR tyrosine kinase inhibitor (EGFR TKI) that targets both EGFR-sensitizing and T790M resistance mutations with IC50 of 0.37 nM (T790M), 0.21 nM (del19/T790M), 0.29 nM(L858R/T790M), and 3.39 nM (EGFR WT).

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5 mg ¥1580 In stock
10 mg ¥2280 In stock
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50 mg ¥5980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Aumolertinib (HS-10296) is a novel, third-generation EGFR tyrosine kinase inhibitor (EGFR TKI) that targets both EGFR-sensitizing and T790M resistance mutations with IC50 of 0.37 nM (T790M), 0.21 nM (del19/T790M), 0.29 nM(L858R/T790M), and 3.39 nM (EGFR WT).
In cell-based assays, almonertinib inhibits EGFR phosphorylation at IC50 of 3.3 nM in HCC827 (EGFR del19) cell line, IC50 of 4.1 nM in PC9 (EGFR del19) cell line, IC50 of 3.3 nM in NCI-H1975 (EGFR L858R/T790M) cell line, but only IC50 of 596.6 nM in A431 (EGFR WT) cell line.

物理化学性质&存储条件

分子量 525.657
分子式 C30H35N7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(5-((4-(1-cyclopropylindol-3-yl)pyrimidin-2-yl)amino)-2-(2-(dimethylamino)ethyl-methylamino)-4-methoxyphenyl)prop-2-enamide

参考文献

1. Yang JC, et al. J Thorac Oncol. 2020 Dec;15(12):1907-1918.

2. Nagasaka M, et al. J Thorac Oncol. 2021 May;16(5):740-763.

3. Wu CP, et al. Biochem Pharmacol. 2021 Jun;188:114516.

4. Lu S, et al. J Thorac Oncol. 2022 Mar;17(3):411-422.

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