N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMSO:100.0(Max Conc. mg/mL);165.67(Max Conc. mM)

form 

Solid

color 

Light yellow to yellow

N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate Usage And Synthesis

Uses

Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects[1][2].

in vivo

IC 50

EGFR L858R: 0.18 nM (IC₅₀); EGFR^T790M: 0.18 nM (IC₅₀); EGFR (WT): 7.68 nM (IC₅₀)

References

[1] Xu X, et al. AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients. Mol Cancer Ther. 2016 Nov;15(11):2586-2597. DOI:10.1158/1535-7163.MCT-16-0281
[2] Yan X, et al. Promising efficacy of novel BTK inhibitor AC0010 in mantle cell lymphoma. J Cancer Res Clin Oncol. 2018;144(4):697-706. DOI:10.1007/s00432-017-2570-8