| CAS NO: | 2158266-58-9 |
| 包装 | 价格(元) |
| 250mg | 电议 |
| 500mg | 电议 |
| Cas No. | 2158266-58-9 |
| Canonical SMILES | O=C(NC)C1=NC=C(C2=CC3=C(C=N2)C(C4=NN(C5CCOCC5)C6=C4CN(C(C)=O)CC6)=CC=C3)C=C1 |
| 分子式 | C29H30N6O3 |
| 分子量 | 510.59 |
| 溶解度 | DMSO: 200 mg/mL (391.70 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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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