Aurora kinase/HDAC-IN-1
Aurora kinase/HDAC-IN-1 is an orally active dual Aurora kinase and HDAC inhibitor that inhibits Aurora A (IC50 = 116 nM), Aurora B (IC50 = 225 nM), HDAC1 (IC50 = 164 nM), and HDAC2 (IC50 = 346 nM).Aurora kinase/HDAC-IN-1 promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis via G2/M cell-cycle arrest. Aurora kinase/HDAC-IN-1 exhibits potent antiproliferative activity in colorectal cancer cells, with an IC50 value of 30.2 nM in HCT-116 cells.Aurora kinase/HDAC-IN-1 significantly suppresses tumor growth in an HCT-116 colorectal cancer xenograft mouse model.
For research use only. We do not sell to patients.
- CAS No.: 2727102-12-5
- Formula: C22H20FN7OS
- Molecular Weight:449.50
-
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]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All Aurora Kinase Isoforms
More
Biological Activity
|
Aurora A 116 nM (IC50) |
Aurora B 225 nM (IC50) |
HDAC1 164 nM (IC50) |
HDAC2 346 nM (IC50) |
Aurora kinase/HDAC-IN-1 (compound 6) (0.64 nM–10 μM; 72 h) inhibits HCT-116 and MIA PaCa-2 cell proliferation with IC50values of 30.2 nM and 42.8 nM, respectively[1].
Aurora kinase/HDAC-IN-1 (30-120 nM; 24 h) induces G2/M arrest in HCT-116 cells[1].
Aurora kinase/HDAC-IN-1 (30-120 nM; 48 h) induces apoptosis in HCT-116 cells[1].
Aurora kinase/HDAC-IN-1 (30-120 nM; 72 h) modulates Aurora/HDAC-related signaling in HCT-116 cells, including increased Ac-H3 and reduced Aurora A phosphorylation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HCT-116 cells; MIA PaCa-2 cells
-
Concentration:0.64 nM-10 μM
-
Incubation Time:72 h
-
Result:Inhibited HCT-116 cell proliferation with an IC50 value of 30.2 nM.
Inhibited MIA PaCa-2 cell proliferation with an IC50 value of 42.8 nM.
-
Cell Line:HCT-116 cells
-
Concentration:30 nM, 60 nM, 120 nM
-
Incubation Time:24 h
-
Result:Increased G2/M-phase population from 5.03% (control) to 12.68% (30 nM), 20.17% (60 nM), and 25.40% (120 nM).
-
Cell Line:HCT-116 cells
-
Concentration:30 nM, 60 nM, 120 nM
-
Incubation Time:48 h
-
Result:Increased apoptosis rate from 1.99% (control) to 21.03% (30 nM), 42.81% (60 nM), and 59.13% (120 nM).
-
Cell Line:HCT-116 cells
-
Concentration:30 nM, 60 nM, 120 nM
-
Incubation Time:72 h
-
Result:Increased Ac-H3 expression and upregulated p53 and Caspase 3 expression, and reduced p-Aurora A levels.
| Species | Dose | Route | CL | Vdss | AUC0-t | T1/2 | Cmax | Tmax | F |
|---|---|---|---|---|---|---|---|---|---|
| Mice | 1 mg/kg | i.v. | 98.6 mL/min/kg | 1.49 L/kg | 168 ng·h/mL | 0.307 h | / | / | / |
| Mice | 50 mg/kg | p.o. | / | / | 1850 ng·h/mL | 5.73 h | 448 ng/mL | 1.00 h | 23.2 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female BALB/c nude mice (6-8 weeks old) bearing subcutaneous HCT-116 xenografts [1]
-
Dosage:50 mg/kg/d, 150 mg/kg/d
-
Administration:Oral gavage (p.o.), once daily (QD), for 21 days.
-
Result:Inhibited tumor growth in HCT-116 colorectal cancer xenograft mice, resulting in a significant reduction in tumor volume without obvious toxicity.
Increased tumor necrosis and reduced Ki67 staining (decreased proliferation), with more pronounced effects at 150 mg/kg/d.
Chemical Information
-
CAS No. 2727102-12-5
-
Molecular Weight 449.50
-
Formula C22H20FN7OS
-
SMILES
O=C(C1=CC=C(CSC2=NC=CC(NC3=NNC(C)=C3)=N2)C=C1)NC4=CC=C(C=C4N)F
-
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)
Aurora kinase/HDAC-IN-1 Related Classifications
HY-179374 Related Classifications
Powered by Bioz