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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 |
|---|
| Phthalazinone pyrazole
Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. |
| Aurora Kinases-IN-4
Aurora Kinases-IN-4 is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). |
| Derrone
Derrone, a prenylated isoflavones, is an Aurora kinase inhibitor, with IC50 values of 6 and 22.3 μM against Aurora B and Aurora A, respectively. Derrone shows anti-tumor activity. |
| CD532 hydrochloride
CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer. |
| Aurora kinase inhibitor-2
Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively. |
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