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 )
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GNE-207
CAS number:2158266-58-9 molecular formula:C29H30N6O3
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2158266-58-9 | molecular formula | C29H30N6O3 |
| molecular weight | 510.59 g/mol | Exact mass | ≥97% |
| PSA | 102.000 Ų | logp | 2.000 |
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