GNE-207是一种有效、选择性、可口服的CBP溴结构域抑制剂，IC50值为1nM，对其选择性是的BRD4(1)的2500多倍，IC50值为3.1μM。在MV-4-11细胞中，GNE-207对MYC表达具有高效活性，EC50值为18nM。
货号:ajcx12912
CAS:2158266-58-9
分子式:C29H30N6O3
分子量：510.59
溶解度:DMSO: 200 mg/mL (391.70 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.