GNE-781 ( GNE781;GNE 781 )

Catalog No. M13035 CAS No. 1936422-33-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GNE-781
Note

Research use only, not for human use.
Brief Description

GNE-781 (GNE781) is a potent, selective, non-CNS penetrant, orally active CBP/p300 bromodomain inhibitor.
Description

GNE-781 (GNE781) is a potent, selective, non-CNS penetrant, orally active CBP/p300 bromodomain inhibitor with IC50 of 0.94/1.2 nM in TR-FRET assays; exhibits high selectivity over BRD4 (1) (>5 uM) and other BRDs; suppresses Myc transcript levels in cellular assays with EC50 of 6.6 nM; displays antitumor activity in an AML tumor model and decreases Foxp3 transcript levels in a dose dependent manner.
Synonyms

GNE781;GNE 781
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

——
Indication

——

CAS Number

1936422-33-1
Formula Weight

525.61
Molecular Formula

C27H33F2N7O2
Purity

>98% (HPLC)
Solubility

DMSO : 100 mg/mL 190.26 mM
SMILES

O=C(N1CCC(N(C2CCOCC2)N=C3N4CCCC5=C4C=C(C(F)F)C(C6=CN(C)N=C6)=C5)=C3C1)NC
Chemical Name

3-[7-(Difluoromethyl)-6-(1-methylpyrazol-4-yl)-3,4-dihydro-2H-quinolin-1-yl]-N-methyl-1-tetrahydropyran-4-yl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide

1. Romero FA, et al. J Med Chem. 2017 Nov 22;60(22):9162-9183.

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