BCL6-IN-8c

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.

Product information

CAS Number: 2130878-25-8

Molecular Weight: 417.84

Formula: C20H20ClN3O5

Chemical Name: 6-{[2-chloro-4-nitro-5-(oxan-4-yloxy)phenyl]amino}-1, 2, 3, 4-tetrahydroquinolin-2-one

Smiles: [O-][N+](=O)C1=CC(Cl)=C(C=C1OC1CCOCC1)NC1C=CC2NC(=O)CCC=2C=1

InChiKey: RRELDGDKULRRDM-UHFFFAOYSA-N

InChi: InChI=1S/C20H20ClN3O5/c21-15-10-18(24(26)27)19(29-14-5-7-28-8-6-14)11-17(15)22-13-2-3-16-12(9-13)1-4-20(25)23-16/h2-3,9-11,14,22H,1,4-8H2,(H,23,25)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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

In Vivo:

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). 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%).

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.

Products are for research use only. Not for human use.