Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib 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 is used for the research of the non-small cell lung cancer.
|Solubility (25°C)||DMSO ≥ 83.33 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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Almonertinib mesylate is an orally active, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR sensitization and T790M resistance mutations, and also shows strong inhibitory activity against T790M, T790M/L858R, and T790M/Del19, with IC50 of 0.37, 0.29, and 0.21 nM, respectively. The IC50 of T790M/Del19 was 0.37, 0.29 and 0.21 nM, respectively, but the inhibitory effect on wild-type was weaker, with an IC50 of 3.39 nM. It can be used in the research of non-small cell lung cancer.
MAPK-IN-2 is a potent MAPK inhibitor with antineoplastic activity.
EGFR-IN-81 is an EGFR inhibitor.
EGFR-IN-85 is an EGFR inhibitor.
JGK-068S is a potent EGFR inhibitor.
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