BCL6 inhibitor 8c( BCL6IN8c | BCL6 inhibitor 8c | BCL6 inhibitor-8c | BCL6 inhibitor8c )

Catalog No. M13392 CAS No. 2130878-25-8

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Product Name

BCL6 inhibitor 8c
Note

Research use only, not for human use.
Brief Description

A novel potent, in vivo-active BCL6 inhibitor with IC50 of 0.1 uM in ELISA assays.
Description

A novel potent, in vivo-active BCL6 inhibitor with IC50 of 0.1 uM in ELISA assays; exhibits good cellular BCL6BTB/ BCoR PPI inhibitory activity in the submicromolar range (M2H IC50=0.72 uM), showed a good pharmacokinetic profile, which is acceptable for both in vitro and in vivo studies.
In Vitro

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.
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%).
Synonyms

BCL6IN8c | BCL6 inhibitor 8c | BCL6 inhibitor-8c | BCL6 inhibitor8c
Pathway

Angiogenesis
Target

Bcl-2
Recptor

Bcl-2
Research Area

——
Indication

——

CAS Number

2130878-25-8
Formula Weight

417.846
Molecular Formula

C20H20ClN3O5
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : ≥ 50 mg/mL (119.66 mM)
SMILES

O=C1NC2=C(C=C(NC3=CC(OC4CCOCC4)=C([N+]([O-])=O)C=C3Cl)C=C2)CC1
Chemical Name

6-((2-Chloro-4-nitro-5-((tetrahydro-2H-pyran-4-yl)oxy)phenyl)amino)-3,4-dihydroquinolin-2(1H)-one

1. Yasui T, et al. Bioorg Med Chem. 2017 Sep 1;25(17):4876-4886.

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