CFON-026 is a selective, orally active non-covalent inhibitor of Bruton’s tyrosine kinase (BTK), exhibiting an IC50 of 0.27 nM. This compound demonstrates substantial antitumor efficacy against both wild-type BTK and various clinically relevant BTK resistance mutations, including C481S, T474I, L528W, and V416L. In vivo studies have shown that CFON-026 induces complete tumor regression in TMD8 xenograft models, making it a valuable tool for investigating hematological malignancies such as chronic lymphocytic leukemia and Waldenström macroglobulinemia.
CFON-026 is a selective, orally active non-covalent inhibitor of Bruton’s tyrosine kinase (BTK), exhibiting an IC50 of 0.27 nM. This compound demonstrates substantial antitumor efficacy against both wild-type BTK and various clinically relevant BTK resistance mutations, including C481S, T474I, L528W, and V416L. In vivo studies have shown that CFON-026 induces complete tumor regression in TMD8 xenograft models, making it a valuable tool for investigating hematological malignancies such as chronic lymphocytic leukemia and Waldenström macroglobulinemia.
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