HCC cell viability and Aurora-associated signaling
Cell-based study · Human Huh-7 and Hep3B hepatocellular carcinoma cell lines [1]
AZD1152-HQPA reduced viable-cell numbers and histone H3 phosphorylation, with altered DNA content and increased sub-G1 fractions. Aurora A phosphorylation was not repressed.
| Endpoint | Reported result | Reference |
|---|---|---|
| Huh-7 viable-cell number after 72 hours | IC50 16.72 ± 2.44 nM | [1] |
| Hep3B viable-cell number after 72 hours | IC50 4.79 ± 1.03 nM | [1] |
| Histone H3 Ser10 and Aurora A Thr288 phosphorylation | Qualitative immunoblot result Histone H3 phosphorylation decreased; Aurora A Thr288 phosphorylation was not repressed. | [1] |
| Hep3B DNA content and Huh-7/Hep3B sub-G1 fractions | Qualitative flow-cytometry result Hep3B accumulated 4N cells at 24 hours and 8N cells at 48 hours; sub-G1 fractions increased with concentration in both lines at 48 hours. | [1] |
Literature-Reported Treatment Conditions
- Treatment concentration
- Viability and immunoblots: 1, 5, 25 and 125 nM. DNA-content/sub-G1 assays: 5, 25 and 125 nM.
- Exposure duration
- Viability: 72 hours; immunoblots: 24 hours; Hep3B DNA content: 24 and 48 hours; sub-G1 fractions: 48 hours.
- Method
- Single-agent exposure; viable-cell counting, immunoblotting and propidium-iodide flow cytometry.
- Vehicle
- DMSO control specified for viability and flow-cytometry experiments; immunoblot control vehicle not explicitly specified.
- Reported limits
- Final DMSO percentage and IC50 fitting method/± definition not reported in the selected text. Figure 4A and Figure 5B identify means ± SD, n = 3; viability methods also describe 3–4 replicates and three repeats, without resolving their nesting.
Methods and source locations
Compound reported in the paper: AZD1152-HQPA; Compound label in the paper: AZD1152-HQPA
Cellular results for the named HQPA compound; no prodrug, nanoparticle, clinical or product-batch equivalence claim.
Results: Anticancer effects of Aurora B kinase selective inhibitor, AZD1152-HQPA, in HCC cells; Figure 4A-B and caption; Methods: Cell culture and reagents, Cell viability and flow cytometry, Western blot analysis; Results: Anticancer effects of Aurora B kinase selective inhibitor, AZD1152-HQPA, in HCC cells; Figure 5A-B and caption; Methods: Cell viability and flow cytometry
Huh-7 viable-cell number after 72 hours: Trypan blue exclusion and hemocytometer counting. Definition of the ± term for the reported IC50 is not explicit. — Results: Anticancer effects of Aurora B kinase selective inhibitor, AZD1152-HQPA, in HCC cells; Figure 4A-B and caption; Methods: Cell culture and reagents, Cell viability and flow cytometry, Western blot analysis
Hep3B viable-cell number after 72 hours: Trypan blue exclusion and hemocytometer counting. Definition of the ± term for the reported IC50 is not explicit. — Results: Anticancer effects of Aurora B kinase selective inhibitor, AZD1152-HQPA, in HCC cells; Figure 4A-B and caption; Methods: Cell culture and reagents, Cell viability and flow cytometry, Western blot analysis
Histone H3 Ser10 and Aurora A Thr288 phosphorylation: Immunoblot after 24 hours; tested concentrations 1, 5, 25 and 125 nM, with control lane. — Results: Anticancer effects of Aurora B kinase selective inhibitor, AZD1152-HQPA, in HCC cells; Figure 4A-B and caption; Methods: Cell culture and reagents, Cell viability and flow cytometry, Western blot analysis
Hep3B DNA content and Huh-7/Hep3B sub-G1 fractions: Propidium-iodide flow cytometry at 5, 25 and 125 nM; vehicle control. No percentages estimated from plotted bars. — Results: Anticancer effects of Aurora B kinase selective inhibitor, AZD1152-HQPA, in HCC cells; Figure 5A-B and caption; Methods: Cell viability and flow cytometry