Aurora kinase/ALK-IN-1
Aurora kinase/ALK-IN-1 is a dual Aurora A kinase and ALK inhibitor with IC50 values of 0.296 μM and 0.332 μM, respectively. Aurora kinase/ALK-IN-1 induces G2/M cell cycle arrest, triggers mitochondrial apoptosis, elevates intracellular reactive oxygen species (ROS) levels, and inhibits ALDH1 activity. Aurora kinase/ALK-IN-1 demonstrates cytotoxicity and tumor selectivity. Aurora kinase/ALK-IN-1 can be used for the research of anaplastic large cell lymphoma.
For research use only. We do not sell to patients.
- Formula: C17H20N6O3S4
- Molecular Weight:484.64
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Aurora Kinase Isoforms
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Biological Activity
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Aurora A 0.296 μM (IC50) |
Aurora B 0.887 μM (IC50) |
Aurora kinase/ALK-IN-1 (compound 22h) (48 h) exhibits potent, selective cytotoxicity against ALK+ ALCL SR cells with an IC50 of 5.10 μM, showing a 7-fold selectivity margin over normal human peripheral blood mononuclear cells[1].
Aurora kinase/ALK-IN-1 (5-10 μM; 24 h) induces dose-dependent depletion of phosphorylated and total Aurora A and ALK in ALK+ ALCL SR cells[1].
Aurora kinase/ALK-IN-1 (5-10 μM; 24 h) induces dose-dependent G2/M cell cycle arrest in ALK+ ALCL SR cells[1].
Aurora kinase/ALK-IN-1 (5-10 μM; 48 h) induces dose-dependent mitochondrial apoptosis in ALK+ ALCL SR cells[1].
Aurora kinase/ALK-IN-1 (5-10 μM; 24 h) elevates intracellular ROS levels in ALK+ ALCL SR cells to 3.5-fold above control levels after 24 h of treatment[1].
Aurora kinase/ALK-IN-1 (24 h) inhibits ALDH1 enzyme activity in ALK+ ALCL SR cell lysates with an IC50 of 2.8 μg/mL, reducing activity by 2.8-fold at 10 μM[1].
Aurora kinase/ALK-IN-1 (5-10 μM; 48 h) synergistically potentiates Ara-C cytotoxicity in ALK+ ALCL SR cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ALK+ ALCL SR cells
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Concentration:5; 10 μM
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Incubation Time:24 h
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Result:Induced a dose-dependent reduction in both phosphorylated and total levels of Aurora A and ALK.
Maintained the ratio of phosphorylated to total protein constant relative to vehicle controls.
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Cell Line:ALK+ ALCL SR cells
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Concentration:5; 10 μM
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Incubation Time:24 h
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Result:Induced a dose-dependent accumulation of cells in the G2/M phase.
Caused a 2.4-fold increase at 5 μM relative to vehicle controls.
Caused a 3.2-fold increase at 10 μM relative to vehicle controls.
Accompanied by reductions in G1 and S phase populations.
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Cell Line:ALK+ ALCL SR cells
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Concentration:5; 10 μM
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Incubation Time:48 h
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Result:Induced a dose-dependent increase in total apoptotic cells.
Resulted in 8.1% total apoptosis at 5 μM relative to ~0.2% in vehicle controls.
Resulted in 17.8% total apoptosis at 10 μM relative to ~0.2% in vehicle controls.
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Cell Line:ALK+ ALCL SR cells
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Concentration:5; 10 μM
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Incubation Time:24 h
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Result:Induced a marked increase in intracellular ROS, reaching 3.5-fold above vehicle control values.
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Cell Line:ALK+ ALCL SR cells, normal human peripheral blood mononuclear cells PCS-800-017
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Concentration:5; 10 μM
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Incubation Time:48 h
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Result:Co-treatment with 10 μM Aurora kinase/ALK-IN-1 reduced the Ara-C IC50 in SR cells from 27.65 μM to 2.15 μM (12.8-fold increase in potency).
Had a Combination Index (CI) of 0.78 indicating synergy.
The combination yielded a selectivity index (SI) of 29.6, representing a 14.1-fold improvement in selectivity over Ara-C alone.
Chemical Information
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Molecular Weight 484.64
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Formula C17H20N6O3S4
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SMILES
S=C(SC(SC(N(C)C)=S)C(C1=C(C)N(C2=CC=C([N+]([O-])=O)C=C2)N=N1)=O)N(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Aurora kinase/ALK-IN-1 Related Classifications
HY-183767 Related Classifications
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- Aurora kinase/ALK-IN-1
- Aurora Kinase
- Anaplastic lymphoma kinase (ALK)
- Mitochondrial Metabolism
- Apoptosis
- Reactive Oxygen Species (ROS)
- Aldehyde Dehydrogenase (ALDH)
- anaplastic large cell lymphoma
- peripheral blood mononuclear cells
- cytarabine
- Aurora A kinase
- ALDH1
- mitochondrial apoptosis
- reactive oxygen species
- G2/M cell cycle arrest
- Cys290
- anaplastic lymphoma kinase
- Inhibitor
- inhibitor
- inhibit