adaphostin

Adaphostin is a small molecule experimental anticancer agent and a member of the tyrphostin family, originally developed as an inhibitor of the Bcr-Abl tyrosine kinase, which is centrally involved in the pathogenesis of chronic myeloid leukemia (CML). Unlike ATP-competitive kinase inhibitors (such as imatinib), adaphostin was designed to inhibit Bcr-Abl by altering the binding site of peptide substrates. However, subsequent research revealed that its principal cytotoxic mechanism is the induction of oxidative stress via the generation of reactive oxygen species (ROS), rather than direct kinase inhibition. Adaphostin induces superoxide and hydrogen peroxide in leukemic and other tumor cells, leading to apoptosis and selective anticancer effects, especially in hematologic malignancies such as CML and acute myeloid leukemia (AML), including imatinib-resistant cases. There is also evidence for activity against certain solid tumors (e.g., non-small cell lung cancer, prostate cancer, glioblastoma). Its activity is linked to mitochondrial dysfunction, activation of redox-sensitive signaling pathways (including Nrf2/HMOX1), and modulation of iron homeostasis[1][4][5][6][2][9].

Other names

NSC 680410NSC680410NSC-680410AG957 adamantyl esterAG-957 adamantyl esterAG 957 adamantyl ester