| Identification | Back Directory | [Name]
BCL6 inhibitor 8c | [CAS]
2130878-25-8 | [Synonyms]
BCL6-IN-8c
BCL6 inhibitor 8c
BCL-6-IN-8c,BCL6IN8c,BCL6 IN 8c
2(1H)-Quinolinone, 6-[[2-chloro-4-nitro-5-[(tetrahydro-2H-pyran-4-yl)oxy]phenyl]amino]-3,4-dihydro- | [Molecular Formula]
C20H20ClN3O5 | [MDL Number]
MFCD34469269 | [MOL File]
2130878-25-8.mol | [Molecular Weight]
417.84 |
| Chemical Properties | Back Directory | [Boiling point ]
625.1±55.0 °C(Predicted) | [density ]
1.410±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 50 mg/mL (119.66 mM) | [form ]
Solid | [pka]
14.28±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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[1]. | [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 (Cmax = 233 ng/mL, Tmax = 2 hours, MRT = 3.3 h, AUC = 1.27 mg h/mL, F (oral bioavailability) = 79.9%)[1]. | [storage]
Store at -20°C | [References]
[1] Yasui T, et al. Discovery of a novel B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor by utilizing structure-based drug design. Bioorg Med Chem. 2017 Sep 1;25(17):4876-4886. DOI:10.1016/j.bmc.2017.07.037 |
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