GNE-207
Names
[ CAS No. ]:
2158266-58-9
[ Name ]:
GNE-207
Biological Activity
[Description]:
GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, a selectively index of >2500-fold against BRD4 (1) (IC50, 3.1 μM)[1]. GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells[1].
[Related Catalog]:
[Target]
CBP:1 nM (IC50)
BRD4(1):3.1 μM (IC50)
[In Vitro]
GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, a selectively index of >2500-fold against BRD4 (1) (IC50, 3.1 μM)[1]. GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells[1].
[In Vivo]
GNE-207 (5 mg/kg) shows moderate clearance in PK, with acceptable oral bioavailability[1].
[References]
[Related Small Molecules]
(+)-JQ1
|
GSK126
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Tazemetostat (EPZ-6438)
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A 485
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ARV-771
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ARV-825
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I-BET762
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BI 2536
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GSK343
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C646
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3-Deazaneplanocin A (hydrochloride)
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I-BET151
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666-15
Chemical & Physical Properties
[ Molecular Formula ]:
C29H30N6O3
[ Molecular Weight ]:
510.59