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GNE-207

CAS number:2158266-58-9    molecular formula:C29H30N6O3

overview

compound introduction

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 cells In Vitro GNE-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 Vivo GNE-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:Solid IC50& Target:BRD4(1) 3.1 μM (IC 50 ) CBP 1 nM (IC 50 )

Specs

Chinese alias-
English alias-
CAS number2158266-58-9molecular formulaC29H30N6O3
molecular weight510.59 g/molExact mass≥97%
PSA102.000 Ųlogp2.000

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