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GNE-272

Chemical Structure : GNE-272

CAS No.: 1936428-93-1

GNE-272 (GNE 272;GNE272)

Catalog No.: PC-60305Not For Human Use, Lab Use Only.

GNE-272 (GNE272) potent and selective the bromodomains of CBP/EP300 inhibitor with IC50 of 0.02 and 0.03 uM for CBP and EP300, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GNE-272 (GNE272) potent and selective the bromodomains of CBP/EP300 inhibitor with IC50 of 0.02 and 0.03 uM for CBP and EP300, respectively.
GNE-272 displays high selectivity over BRD4 (1) and other BRDs (>10 uM).
GNE-272 shows antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo.
GNE-272 exhibits excellent in vivo PK and antitumor activity in an AML tumor model.

Physicochemical Properties

M.Wt 424.48
Formula C22H25FN6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

References

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

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