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编 号:F272135
分子式:C20H20ClN3O5
分子量:417.84
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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生物活性:
TP-021 (BCL6-IN-8c) is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 μM in cell-free enzyme-linked immunosorbent assay.

体内研究:
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 (Cmax = 233 ng/mL, Tmax = 2 hours, MRT = 3.3 h, AUC = 1.27 mg?h/mL, F (oral bioavailability) = 79.9%).

体外研究:
TP-021 (BCL6-IN-8c, Compound 8c) also exhibits good cellular PPI inhibitory activity in the submicromolar range (M2H IC50 = 0.72 μM). TP-021 (BCL6-IN-8c) does not exhibit significant cytotoxicity even at 30 μM.
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