OICR12694 (OICR 12694, JNJ-65234637) is a potent, selective, and orally bioavailable BCL6-BTB inhibitor with SPR KD value of 5 nM.
OICR12694 showed >100-fold binding selectivity toward other BTB proteins, including BAZF, MIZ1, PLZF, FAZF, Kaiso, and LRF.
OICR12694 also exhibited minimal inhibitory activity against a panel of diverse kinases (Eurofins 109 kinome panel profile at 1 uM).
OICR12694 showed a potent growth suppression of BCL6-dependent cell lines such as Karpas-422 (IC50=92 nM) and potent antiproliferative activity (SUDHL4 Luc, EC50 =89 nM).
OICR12694 exhibited low clearance and good oral exposure in mice and dogs, did not impair the function of various cytochrome P450 (CYPs) isoforms in vitro.
