GNE-207 (C007B-357134)

GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP , with an IC 50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC 50 of 18 nM for MYC expression in MV-4-11 cellsIn VitroGNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC 50 of 1 nM, a selectively index of >2500-fold against BRD4 (1) (IC 50 , 3.1 μM). GNE-207 shows excellent CBP potency, with an EC 50 of 18 nM for MYC expression in MV-4-11 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoGNE-207 (5 mg/kg) shows moderate clearance in PK, with acceptable oral bioavailability . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:BRD4(1) 3.1 μM (IC 50 ) CBP 1 nM (IC 50 ).

Specifications and Purity: ≥97%

Molecular Formula: C29H30N6O3

Molecular Weight: 510.59

PubChem CID: 132186469

Isomeric SMILES: CC(=O)N1CCC2=C(C1)C(=NN2C3CCOCC3)C4=CC=CC5=CC(=NC=C54)C6=CN=C(C=C6)C(=O)NC