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Chemical Structure : OICR12694
Catalog No.: PC-49791Not For Human Use, Lab Use Only.
OICR12694 (OICR 12694, JNJ-65234637) is a potent, selective, and orally bioavailable BCL6-BTB inhibitor with SPR KD value of 5 nM.
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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.
| M.Wt | 645.04 | |
| Formula | C29H28ClF3N8O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Ahmed Mamai, et al. ACS Medicinal Chemistry Letters 2023, 14, 2, 199-210.
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