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DGN462 is a highly potent cytotoxic small molecule belonging to the indolino-benzodiazepine (IGN) dimer class, specifically designed by ImmunoGen as a payload for antibody-drug conjugates (ADCs). It functions as a DNA-alkylating agent that binds to the minor groove of DNA, leading to DNA damage and apoptosis in target cells. DGN462 is characterized as an indolino-benzodiazepine dimer containing a mono-imine moiety. It is the cytotoxic component of IMGN779, an ADC targeting CD33, which has been investigated for the treatment of acute myeloid leukemia (AML), including cases with FLT3-ITD mutations. Unlike some other benzodiazepine dimers that cause DNA cross-linking, DGN462 is a mono-imine alkylator, which may offer a different toxicity profile while maintaining high potency against multi-drug resistant cells.
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