GNE-272 ( GNE 272;GNE272 )

Catalog No. M13036 CAS No. 1936428-93-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GNE-272
Note

Research use only, not for human use.
Brief Description

A potent and selective the bromodomains of CBP/EP300 inhibitor with IC50 of 0.02 and 0.03 uM for CBP and EP300, respectively.
Description

A potent and selective the bromodomains of CBP/EP300 inhibitor with IC50 of 0.02 and 0.03 uM for CBP and EP300, respectively; displays high selectivity over BRD4 (1) and other BRDs (>10 uM); shows antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo; exhibits excellent in vivo PK and antitumor activity in an AML tumor model.
Synonyms

GNE 272;GNE272
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

Cancer
Indication

——

CAS Number

1936428-93-1
Formula Weight

424.48
Molecular Formula

C22H25FN6O2
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 150 mg/mL 353.38 mM
SMILES

CC(N1CCC2=C(C(NC3=C(F)C=C(C4=CN(C)N=C4)C=C3)=NN2[C@H]5CCOC5)C1)=O
Chemical Name

(S)-1-(3-((2-Fluoro-4-(1-methyl-1H-pyrazol-4-yl)phenyl)amino)-1-(tetrahydrofuran-3-yl)-6,7-dihydro-1H-pyrazolo[4,3-c]pyridin-5(4H)-yl)ethanone

1. Crawford TD, et al. J Med Chem. 2016 Dec 8;59(23):10549-10563.

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