CCT374705

**CCT374705** is an orally active small molecule inhibitor of B-cell lymphoma 6 (BCL6) transcription factor with an IC50 of 4.8 nM in biochemical assays and potent antiproliferative effects in BCL6-dependent lymphoma cell lines such as Karpas 422 and OCI-Ly1 (GI50 <100 nM). Developed by researchers at The Institute of Cancer Research (ICR), it features a tricyclic quinolinone scaffold with 5-chloro-6-fluoropyridine substitution, optimized for favorable pharmacokinetic properties including moderate oral bioavailability (48% in mice), low microsomal clearance, good permeability, and sustained in vivo exposure. CCT374705 demonstrated modest antitumor efficacy in a Karpas 422 lymphoma xenograft mouse model upon oral dosing (50 mg/kg BID), with a clean selectivity profile across 78 targets and 468 kinases.