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.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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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 binds to CRBNmidi, with a measured Kd value of 97 nM determined by MST at 25 °C[1].
Abd141 (10 nM-5 μM; 24 h) potently degrades ATR (DC50 = 97.7 nM) and Aurora A (DC50 = 6.7 nM) after 24-hour incubation in MOLT-4 acute lymphoblastic leukemia cells, and does not affect the level of WEE1 at a concentration of 500 nM[1].
Abd141 (0.5 μM; 24-120 h) inhibits the proliferation of MOLT-4 acute lymphoblastic leukemia cells in a CRBN-dependent manner[1].
Abd141 (0.5 μM; 24 h) enhances Cytarabine (HY-13605)-induced apoptosis of MOLT-4 acute lymphoblastic leukemia cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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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.
Protocole
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Abd141 Related Classifications
HY-187195 Related Classifications
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