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Almonertinib

Chemical Structure : Almonertinib

CAS No.: 1899921-05-1

Almonertinib (HS-10296)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 525.657
Formula C30H35N7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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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