Avitinib maleate dihydrate  (Synonyms: Abivertinib maleate dihydrate; AC0010 maleate dihydrate)

Avitinib (Abivertinib) maleate dihydrate 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 dihydrate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate dihydrate shows anticancer effects^[1][2].

Avitinib maleate dihydrate (AC0010; 0.13 nM-2 μM; 2 h) selectively inhibits mutant EGFR phosphorylation with IC₅₀ values of 7.3 and 2.8 nM in NCI-H1975 and NIH/3T3_TC32T8 cells, about 115- and 298-fold more sensitive than that of the inhibition of wild-type EGFR in A431. Avitinib maleate dihydrate potently inhibits EGFR-Tyr1068 phosphorylation in NCI-H1975 cells, and the selectivity ratio is at 65-fold for NCI-H1975 cells versus A431 cells. In addition to inhibition of EGFR-Tyr1068 phosphorylation, Avitinib maleate dihydrate inhibits phosphorylation of the downstream targets Akt and ERK1/2 in NCI-H1975 and HCC827 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Avitinib maleate dihydrate (AC0010; 12.5-500 mg/kg; orally administration; once daily; for 14 days) inhibits EGFR-mutant tumor growth but not wild-type EGFR tumor growth in xenograft models over extended duration^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

639.63

C₃₀H₃₄FN₇O₈

1822357-78-7

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Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [2]. Yan X, et al. Promising efficacy of novel BTK inhibitor AC0010 in mantle cell lymphoma. J Cancer Res Clin Oncol. 2018 Apr;144(4):697-706.  [Content Brief]