GNE-207( GNE207 | GNE 207 )

Catalog No. M13443 CAS No. 2158266-58-9

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GNE-207
Note

Research use only, not for human use.
Brief Description

GNE-207 (GNE207) is a novel potent, selective, orally active CBP/p300 bromodomain with IC50 of 1.0 nM.
Description

GNE-207 (GNE207) is a novel potent, selective, orally active CBP/p300 bromodomain with IC50 of 1.0 nM; displays >2,500-fold selectivity over BRD4; suppresses Myc transcript levels in MV-4-11 cellular assays with EC50 of 18 nM; exhibits a good pharmacokinetic profile.
In Vitro

GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, a selectively index of?>2500-fold against BRD4 (1) (IC50, 3.1 μM).GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
In Vivo

GNE-207 (5?mg/kg) shows moderate clearance in PK, with acceptable oral bioavailability.
Synonyms

GNE207 | GNE 207
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

——
Indication

——

CAS Number

2158266-58-9
Formula Weight

510.598
Molecular Formula

C29H30N6O3
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 200 mg/mL (391.70 mM)
SMILES

O=C(NC)C1=NC=C(C2=CC3=C(C=N2)C(C4=NN(C5CCOCC5)C6=C4CN(C(C)=O)CC6)=CC=C3)C=C1
Chemical Name

5-(8-(5-acetyl-1-(tetrahydro-2H-pyran-4-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)isoquinolin-3-yl)-N-methylpicolinamide

1. Lai KW, et al. Bioorg Med Chem Lett. 2018 Jan 1;28(1):15-23.

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