Aurora kinase-IN-8
Aurora kinase-IN-8 is a orally active Aurora kinase inhibitor. Aurora kinase-IN-8 shows IC50 values of 2.8 and 28.1 nM against Aurora A kinase and Aurora B kinase. Aurora kinase-IN-8 can prevent spindle formation, cause G2/M phase arrest, and induce cell apoptosis. Aurora kinase-IN-8 can be used for the research of cancer, such as triple-negative breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 1911629-44-1
- Formula: C25H27N7
- Molecular Weight:425.53
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Aurora Kinase Isoforms
More
Biological Activity
|
Aurora A 2.8 nM (IC50) |
Aurora B 28.1 nM (IC50) |
Aurora kinase-IN-8 (Compound 9h) demonstrates superior activity against MDA-MB-231 cells with an IC50 value of 48 nM and 40-560 nM against other cancer cells[1].
Aurora kinase-IN-8 (1 μM, 48 h) inhibits Aurora A kinase phosphorylation in MDA-MB-231 cells[1].
Aurora kinase-IN-8 (1 μM, 48 h) prevents spindle formation in MDA-MB-231 cells[1].
Aurora kinase-IN-8 (0.3-1.2 μM, 24 h) induces G2/M phase arrest and apoptosis in MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MDA-MB-231 cells
-
Concentration:1 μM
-
Incubation Time:48 h
-
Result:Inhibited Aurora A kinase phosphorylation.
-
Cell Line:MDA-MB-231 cells
-
Concentration:0.3 and 0.6 μM
-
Incubation Time:24 h
-
Result:Caused cell cycle G2/M phase arrest and aneuploidy.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:MDA-MB-231 xenograft tumor mice models[1]
-
Dosage:30 mg/kg
-
Administration:Orally gavage, every 2 days for 19 days
-
Result:Showed a tumor growth inhibition (TGI) rate of 59%.
Reduced tumor weight and volume.
Had no significant impact on mouse body weight and liver/lung weight.
Chemical Information
-
CAS No. 1911629-44-1
-
Molecular Weight 425.53
-
Formula C25H27N7
-
SMILES
CN(CC1)CCN1C(C=C2)=CC3=C2C(NC4=NNC(C)=C4)=NC(/C=C/C5=CC=CC=C5)=N3
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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)