DOT1L808 is a potent and highly selective DOT1L PROTAC degrader with a DC50 value of 5 nM. DOT1L808 can promote the ubiquitination and degradation of DOT1L. DOT1L808 exhibits antitumor activity in an orthotopic leukemia model [1]. (Pink: DOT1L ligand; Blue: VHL ligand; Black: linker).
In Vivo, DOT1L808 (25 mg/kg; i.p.; twice daily; 5 days per week for 2 weeks) significantly inhibits tumor growth in the MV-4−11-Luc acute myeloid leukemia model of NSG mice[1].
References:
[1]. Quan S, et al. Development of DOT1L-Targeted Protein Degraders for Treating MLL-r Leukemia. J Med Chem. 2026;69(4):4439-4468.
In Vivo, DOT1L808 (25 mg/kg; i.p.; twice daily; 5 days per week for 2 weeks) significantly inhibits tumor growth in the MV-4−11-Luc acute myeloid leukemia model of NSG mice[1].
References:
[1]. Quan S, et al. Development of DOT1L-Targeted Protein Degraders for Treating MLL-r Leukemia. J Med Chem. 2026;69(4):4439-4468.