2-Propenamide, N-[5-[[4-(1-cyclopropyl-1H-indol-3-yl)-2-pyrimidinyl]amino]-2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxyphenyl]-, compd. with methanesulfonate (1:1) Chemical Properties

storage temp. 

4°C, away from moisture

solubility 

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

form 

Solid

color 

Light yellow to yellow

2-Propenamide, N-[5-[[4-(1-cyclopropyl-1H-indol-3-yl)-2-pyrimidinyl]amino]-2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxyphenyl]-, compd. with methanesulfonate (1:1) Usage And Synthesis

Uses

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].

References

[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 DOI:10.1016/j.jtho.2020.09.001
[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. DOI:10.3389/fmed.2016.00076