OICR12694 | Bcl-6 BTB inhibitor | Probechem Biochemicals

Chemical Structure : OICR12694

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OICR12694 (JNJ-65234637)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	645.04
分子式	C29H28ClF3N8O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-5-(1-(2-((3-chloro-6-(2,4-dimethylpiperazin-1-yl)-2-fluoropyridin-4-yl)amino)-2-oxoethyl)-4-oxo-4,6,7,8-tetrahydro-1H-dipyrrolo[1,2-a:2',3'-d]pyrimidin-3-yl)-3,4-difluoro-2-hydroxybenzamide

参考文献

1. Ahmed Mamai, et al. ACS Medicinal Chemistry Letters 2023, 14, 2, 199-210.

OICR12694 (JNJ-65234637)

生物&药学活性

物理化学性质&存储条件

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OICR12694 (JNJ-65234637)

生物&药学活性

物理化学性质&存储条件

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