产品描述
BCL6-IN-8c is an orally active and potent inhibitor of B-cell lymphoma 6 (BCL6)-corepressor interaction(IC50 of 0.10 μM in cell-free enzyme-linked immunosorbent assay).
体外活性
BCL6-IN-8c (Compound 8c) exhibits good cellular PPI inhibitory activity in the submicromolar range (M2H IC50 = 0.72 μM). BCL6-IN-8c can not exhibit significant cytotoxicity even at 30 μM[1].
体内活性
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%)[1]. The pharmacokinetic profile of BCL6-IN-8c (Compound 8c) is evaluated by a mouse cassette-dosing study (0.1 mg/kg iv; 1 mg/kg po).
Cas No.
2130878-25-8
分子式
C20H20ClN3O5
分子量
417.84
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years