TP-021 (BCL6-IN-8c) is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC 50 of 0.10 µM in cell-free enzyme-linked immunosorbent assay
In Vitro
TP-021 (BCL6-IN-8c, Compound 8c) also exhibits good cellular PPI inhibitory activity in the submicromolar range (M2H IC 50 = 0.72 µM). TP-021 (BCL6-IN-8c) does not exhibit significant cytotoxicity even at 30 µM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The pharmacokinetic profile of TP-021 (BCL6-IN-8c, Compound 8c) is evaluated by a mouse cassette-dosing study (0.1 mg/kg iv; 1 mg/kg po). TP-021 (BCL6-IN-8c) exhibits a good pharmacokinetic profile (C max = 233 ng/mL, T max = 2 hours, MRT = 3.3 h, AUC = 1.27 mg•h/mL, F (oral bioavailability) = 79.9%) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.