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CAS号 | 1936422-33-1 | 货号 | BCP29560 |
中文名 | GNE-781 | ||
英文名 | GNE-781 | ||
中文别名 | |||
英文别名 | GNE 781; GNE781; | ||
SMILES | O=C(N1CCC(N(C2CCOCC2)N=C3N4CCCC5=C4C=C(C(F)F)C(C6=CN(C)N=C6)=C5)=C3C1)NC | ||
化学名称 | |||
分子式 | C27H33F2N7O2 | 分子量 | 525.60 |
纯度 | 98% | 配送 | 惯例下常温包邮 |
产品描述 | GNE-781 is a Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) . GNE-781 showed TR-FRET IC50 = 0.94 nM, BRET IC50 = 6.2 nM, BRD4(1) IC50 = 5,100 nΜ) that maintained good in vivo PK properties in multiple species. GNE-781 displays anti-tumor activity in an AML tumor model and was also shown to decrease Foxp3 transcript levels in a dose dependent manner. |
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