| Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2417371-71-0 | [Synonyms]
| [Molecular Formula]
C56H67F2N9O8S2 | [Molecular Weight]
1096.31 |
| Chemical Properties | Back Directory | [Boiling point ]
1261.9±65.0 °C(Predicted) | [density ]
1.40±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
14.08±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC)[1]. | [IC 50]
BRD4 (BD1): 4.7 nM (IC50); BRD4 (BD2): 4.4 nM (IC50); VHL | [References]
[1] Pillow TH, et al. Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity. ChemMedChem. 2019 Oct 31. DOI:10.1002/cmdc.201900497 |
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| Company Name: |
csynbio
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| Tel: |
15051477682 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList1949820/0_EN.htm |
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