GNE-781
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CAS No. | 1936422-33-1 | Cat. No. | BCP29560 |
Name | GNE-781 | ||
Synonyms | 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 | ||
Chemical Name | |||
Formula | C27H33F2N7O2 | M. Wt | 525.60 |
Purity | 98% | Storage | Store at 4-8°C |
Description | 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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