GNE-207 |
| カタログ番号GC33212 |
GNE-207 は、1 nM の IC50 を持つ CBP のブロモドメインの強力で選択的な経口生物学的利用可能な阻害剤であり、BRD4 に対して >2500 倍の選択的指数を示します (1)。 GNE-207 は、MV-4-11 細胞における MYC 発現の EC50 が 18 nM で、優れた CBP 効力を示します。
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Cas No.: 2158266-58-9
Sample solution is provided at 25 µL, 10mM.
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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].
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].
GNE-207 (5mg/kg) shows moderate clearance in PK, with acceptable oral bioavailability[1].
[1]. Lai KW, et al. Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300. ioorg Med Chem Lett. 2018 Jan 1;28(1):15-23.
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