1557267-42-1

Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It is selective for EGFR-active and T790M mutations, exhibiting a 298-fold increase in potency compared with wild-type EGFR. In a xenograft model, oral administration of 500 mg/kg avitinib was shown to result in complete remission of tumors with EGFR-active and T790M mutations.

Abivertinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). Abivertinib synergistically strengthens anti-leukemia activity of venetoclax in acute myeloid leukemia in BTK-dependent manner.

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

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[1] XIAO XU. AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients.[J]. Molecular Cancer Therapeutics, 2016, 15 11: 2586-2597. DOI: 10.1158/1535-7163.mct-16-0281