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CYC116 is a potent, small molecule inhibitor of Aurora A, B and C with IC50 value of 44, 19 and 65 nM respectively. Additionally, CYC116 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2) kinase in vitro (IC50= 69 nM). CYC-116 shows potent antiproliferative activity against cancer cell lines with with IC50s of 0.599, 0.59, 0.241, 0.34, 0.725, 1.375, 0.471, 0.034, 0.372, 0.681, 0.151, 1.626, 0.775, 0.308, 0.110, 0.09 for MCF7, HeLa, Colo205, HCT-116, HT29, K562, CCRF-CEM, MV4-11, HL60, NCI-H460, A2780, BxPC3, HuPT4, Mia-Paca-2, Saos-2, Messa cells. CYC116 has antitumor activity in various solid tumor and leukemia xenograft model.
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Source | Chin J Integr Med (2015). Figure 5. CYC116 |
| Method | Flow Cytometry Detection of Apoptosis | |
| Cell Lines | RPMI8226 Cell | |
| Concentrations | 0.5 mg/L | |
| Incubation Time | 24 h | |
| Results | For treatment with matrine or CYC116 alone, early apoptosis rates were 1.91% and 2.38%, respectively. However, the early apoptosis rate following combined drug treatment was 9.25%, indicating a synergistic effect of matrine and CYC116 on the induction of apoptosis in MM cells. |
| Cell Experiment | |
|---|---|
| Cell lines | HeLa, MCF7, MV4-11 and A2780 cells line |
| Preparation method | Cell Viability Assay. Inhibition of cell growth was measured by a standard MTT (thiazolyl blue; 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay using a panel of tumor cell lines.Briefly: cells were seeded (2,500–5,000 cells/well) in 96-well plates and allowed to attach for ~ 24 h. Cells were incubated with test compounds for 96 h in DMEM medium containing 10% fetal bovine serum. Cells were treated with a range of compound concentrations in triplicate to generate dose-response curves. The compound concentration required to inhibit 50% of cell growth (IC50) was determined using nonlinear regression analysis. |
| Concentrations | 0~10 μ M |
| Incubation time | 96 h |
| Animal Experiment | |
|---|---|
| Animal models | Murine P388/D1 Leukemia Model (1) / Murine NCI-H460 non-small cell lung cancer xenograft model (2) |
| Formulation | DMSO/ddH20 |
| Dosages | 45 or 67mg/kg twice daily on days 1-3 and 7-9(1) / 75 and 100mg/kg once daily starting on day 1 and for 5 days(2) |
| Administration | oral gavage |
| Molecular Weight | 368.46 |
| Formula | C18H20N6OS |
| CAS Number | 693228-63-6 |
| Solubility (25°C) | DMSO 12 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Aurora Kinase Products |
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| AZD1152-HQPA
AZD1152-HQPA (Barasertib) is a highly potent and selective inhibitor of Aurora with Ki values of 0.36 and 1369 nM for Aurora B and Aurora A respectively. |
| CCT-129202
CCT129202 is an Aurora kinase inhibitor with IC50 of 0.042 ± 0.022, 0.198 ± 0.05, and 0.227 ± 0.064 μmol/L for Aurora A, Aurora B, and Aurora C, respectively. |
| ENMD-2076
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| MLN8054
MLN8054 is an orally bioavailable, highly selective small molecule inhibitor of Aurora with IC50s of 0.004uM and 0.172uM. for Aurora A and Aurora B. |
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