AB3067
AB3067 is a PROTAC degrader for BET protein, that recruits two different E3 ligase Cereblon and VHL with good affinity (IC50=559 nM for VHL in live HEK293; IC50=190 nM for CRBN in live HEK293), and degrades BRD2, BRD3, BRD4 and CRBN with DC50 of 2.1~2.3, 1.6, 15 and 75 nM, respectively. AB3067 inhibits the proliferation of RKO cell with an EC50 of 111 nM.
(Pink: BET ligand (HY-131633A) and no Target protein ligand; Blue: Cereblon ligand (HY-W998346) and VHL ligand (HY-112078); Black: linker and linker).
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- Formule: C74H91ClFN11O17S2
- Masse moléculaire:1525.16
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
|
BRD3 1.6 nM (DC50) |
BRD2 2.1 nM (DC50) |
BRD4 15 nM (DC50) |
Chemical Information
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Masse moléculaire 1525.16
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Formule C74H91ClFN11O17S2
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SMILES
O=C(OCCOCCOCCOCC(C)(COCCOCCOCCNC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2=O)=O)C=C1F)COCC(N[C@H](C(N4[C@H](C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)C[C@@H](O)C4)=O)C(C)(C)C)=O)C[C@H]7C8=NN=C(C)N8C9=C(C(C)=C(C)S9)C(C%10=CC=C(Cl)C=C%10)=N7
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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