Almonertinib (hydrochloride)

Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride 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 hydrochloride is used for the research of the non-small cell lung cancer[1][2].

Product Specifications

CAS Number

[2134096-03-8]

Product Name Alternative

HS-10296 (hydrochloride)

UNSPSC

12352005

Hazard Statement

H315, H317, H319, H335

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/HS-10296_hydrochloride.html

Purity

98.92

Solubility

DMSO : 5 mg/mL (ultrasonic) |H2O : 12.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

COC(C=C(N(C)CCN(C)C)C(NC(C=C)=O)=C1)=C1NC2=NC(C3=CN(C4CC4)C5=C3C=CC=C5)=CC=N2.[H]Cl

Molecular Formula

C30H36ClN7O2

Molecular Weight

562.11

Precautions

H315, H317, H319, H335

References & Citations

[1]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.|[2]Wu SG, et al. Management of acquired resistance to EGFR TKI-targeted therapy in advanced non-small cell lung cancer. Mol Cancer. 2018 Feb 19;17 (1) :38.|[3]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; S1556-0864 (20) 30714-0.