Abd141
Abd141 is a dual PROTAC degrader of ATR and Aurora kinase A (AURKA), with DC50 values of 97.7 nM and 6.7 nM, respectively. Abd141 inhibits the proliferation of acute lymphoblastic leukemia cells. Abd141 can be used in the research of acute lymphoblastic leukemia.
(Pink: AURKA and ATR ligand (HY-187196); Blue: Cereblon ligand (HY-43722); Black: linker).
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- Formule: C43H44N8O7S
- Masse moléculaire:816.92
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
[1]|
Aurora A 6.7 nM (DC50) |
ATR 97.7 nM (DC50) |
Cereblon 97 nM (Kd) |
In Vitro
Abd141 (0.5 μM; 24-120 h) inhibits the proliferation of MOLT-4 acute lymphoblastic leukemia cells in a CRBN-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLT-4 wild-type and MOLT-4ΔCRBN cells
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Concentration:0.5 μM
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Incubation Time:24 h, 96 h, 120 h
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Result:Stalled MOLT-4 wild-type cell growth, with significantly lower cell numbers at 96 h and 120 h compared to untreated controls.
Showed no growth suppression in MOLT-4ΔCRBN cells.
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Cell Line:MOLT-4 cells
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Concentration:0.5 μM Abd141; 0.5 μM Cytarabine
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Incubation Time:24 h
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Result:Did not induce significant apoptosis when used alone.
Augmented Cytarabine-induced apoptosis from 34% to 62%.
Chemical Information
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Masse moléculaire 816.92
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Formule C43H44N8O7S
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SMILES
O=C(C1=NC(C2=CC=C(S(=O)(NCCC3CCN(C(CCCC#CC4=CC=CC5=C4CN(C(CC6)C(NC6=O)=O)C5=O)=O)CC3)=O)C=C2)=CN=C1N)NC7=CC=CC=C7
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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)