[1,4]Oxazepino[2,3-c]quinolin-6(7H)-one, 10-[[5-chloro-2-[(3R,5S)-3-hydroxy-5-methyl-1-piperidinyl]-4-pyrimidinyl]amino]-2-cyclopropyl-3,3-difluoro-1,2,3,4-tetrahydro-7-methyl-, (2S)-

CCT373566 is a highly potent BCL6 degrader (IC50 =0.7 nM) suitable for sustained depletion of BCL6 in vivo. CCT373566 showed modest in vivo efficacy in a lymphoma xenograft mouse model following oral dosing. The transcriptional repressor BCL6 is an oncogenic driver found to be deregulated in lymphoid malignancies.

The antiproliferative activity of the degrader CCT373566 and the inhibitor CCT373567 was tested in a panel of cell lines (Table 5). The degradation of BCL6 by CCT373566 translated into potent antiproliferative activity._x000D_ _x000D_ Reference: J Med Chem. 2022 Jun 23;65(12):8191-8207. https://pubmed.ncbi.nlm.nih.gov/35653645/

CCT373566 is a potent and orally active degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM.