AURKA-IN-5
AURKA-IN-5 is a potent irreversible covalent AURKA inhibitor with an IC50 of 4.94 nM. AURKA-IN-5 RA2 covalently binds to the intrinsic arginine residue Arg220 in the AURKA kinase domain through its CNBA warhead, thereby competitively inhibiting AURKA activity. AURKA-IN-5 can be used for research on leukemia.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C27H17ClFN5O2
- Masse moléculaire:497.91
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Voir tous les produits spécifiques à Isoform Aurora Kinase
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Activité biologique
Description
IC50 & Target
[1]|
Aurora A 4.94 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | GI50 |
> 2000 nM
|
Antiproliferative activity against human CCRF-CEM leukemia cells assessed as viability reduction incubated 72 hrs by CCK-8 assay with GI50 greater than 2000 nM.
Antiproliferative activity against human CCRF-CEM leukemia cells assessed as viability reduction incubated 72 hrs by CCK-8 assay with GI50 greater than 2000 nM.
|
42911680 |
| HL-60 | GI50 |
> 2000 nM
|
Antiproliferative activity against human HL-60 leukemia cells assessed as viability reduction incubated 72 hrs by CCK-8 assay with GI50 greater than 2000 nM.
Antiproliferative activity against human HL-60 leukemia cells assessed as viability reduction incubated 72 hrs by CCK-8 assay with GI50 greater than 2000 nM.
|
42911680 |
In Vitro
AURKA-IN-5 (10 μM; 120 min) has very low cell membrane permeability in Caco-2 cells, with a Papp of 0.12 × 10-6 cm/s[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 497.91
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Formule C27H17ClFN5O2
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SMILES
N#CC1=CC(NC2=NC=C3C(C4=CC=C(Cl)C=C4C(C5=C(OC)C=CC=C5F)=NC3)=N2)=CC=C1C=O
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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)