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sFGN849 is a small molecule indolinobenzodiazepine pseudodimer (IGN) that acts as a DNA-alkylating agent. It is the free payload component of the antibody-drug conjugate pivekimab sunirine (IMGN632), which targets CD123. sFGN849 exerts its cytotoxic effect by binding to the minor groove of DNA and forming covalent alkylating adducts, leading to DNA damage and cell death. Preclinical studies have demonstrated that its activity is significantly modulated by TP53 status and the expression of anti-apoptotic BCL-2 family proteins, while it remains relatively unaffected by common ABC transporter proteins such as P-glycoprotein or BCRP. It is primarily utilized in research to characterize the mechanism of action and resistance profiles of IGN-containing therapeutic assets.
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