| Identification | Back Directory | [Name]
GNE-781 | [CAS]
1936422-33-1 | [Synonyms]
GNE-781
3-(7-(difluoromethyl)-6-(1-methyl-1H-pyrazol-4-yl)-3,4-dihydroquinolin-1(2H)-yl)-N-methyl-1-(tetrahydro-2H-pyran-4-yl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
5H-Pyrazolo[4,3-c]pyridine-5-carboxamide, 3-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-1,4,6,7-tetrahydro-N-methyl-1-(tetrahydro-2H-pyran-4-yl)- | [Molecular Formula]
C27H33F2N7O2 | [MDL Number]
MFCD31693834 | [MOL File]
1936422-33-1.mol | [Molecular Weight]
525.59 |
| Chemical Properties | Back Directory | [Melting point ]
135-140oC | [Boiling point ]
800.7±65.0 °C(Predicted) | [density ]
1.45±0.1 g/cm3(Predicted) | [storage temp. ]
Refrigerator | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
14.19±0.20(Predicted) | [color ]
White to Pale Yellow |
| Hazard Information | Back Directory | [Uses]
GNE-781 is a highly advanced, potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein, binding protein (CBP). Inhibition of the bromodomain of the transcriptional regulator CBP/P300 is an especially interesting new therapeutic approach in oncology. | [in vivo]
GNE-781 (3-30 mg/kg; p.o.; twice daily for 21 days) has tumor growth inhibition (%TGI) is 73%, 71%, and 89% at 3, 10, and 30 mg/kg, respectively in SCID beige mice with MOLM-16 AML xenografts[1].
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GNE-781 decreases Foxp3 transcript levels in a dose dependent manner. GNE-781 (3-30 mg/kg) suppresses MYC at doses as low as 3 mg/kg at 2 and 8 h, with maximal suppression at 10 and 30 mg/kg at 2 h (87% and 88% inhibition, respectively)[1].
| [storage]
Store at -20°C |
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| Company Name: |
DC Chemicals
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021-58447131 13564518121 |
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http://m.approvedhomemanagement.com/ShowSupplierProductsList927327/0.htm |
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