| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C18H20N6OS |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
CYC-116 is a potent inhibitor of Aurora A and Aurora B, with Ki values of 8 nM and 9 nM, respectively. It is supplied as a light yellow to yellow solid (C18H20N6OS, MW 368.46) at 99.05% purity.
Physical & Chemical Properties
| CAS Number | 693228-63-6 |
|---|---|
| Molecular Formula | C18H20N6OS |
| Molecular Weight | 368.46 g/mol |
| Purity | 99.05% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | CC1=C(SC(N)=N1)C2=NC(NC3=CC=C(C=C3)N4CCOCC4)=NC=C2 |
| Target | Aurora A, Aurora B |
| Signaling Pathway | Cell Cycle/DNA Damage; Epigenetics |
| Solubility | In Vitro: DMSO: 15 mg/mL (40.71 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: < 0.1 mg/mL (insoluble) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
Aurora A 8 nM (Ki) |
Aurora B 9.2 nM (Ki) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 15 mg/mL (40.71 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | < 0.1 mg/mL | insoluble |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | 1.5 mg/mL (4.07 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 1.5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (15.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 1.5 mg/mL (4.07 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (15.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vitro
VEGFR2, Src, Lck and FLT3 are also inhibited by CYC-116, with Kis of 44, 82, 280, 44 nM, respectively. Broad-spectrum antitumor activity may be a property of CYC-116. Potent antiproliferative activity against cancer cell lines is displayed by CYC-116, 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 and HT29 cells, K562 and CCRF-CEM cells, MV4-11, HL60, NCI-H460 and A2780 cells, plus BxPC3, HuPT4, Mia-Paca-2, Saos-2 and Messa cells. Complete inhibition of histone H3 phosphorylation in HeLa cell lysates results from treatment with CYC-116 at 1.25 μM for 7 h[1].
In Vivo
Oral CYC-116 at 75 and 100 mg/kg q.d. produces tumor growth delays of 2.3 and 5.8 days, corresponding to specific growth delays of 0.32 and 0.81, respectively. Throughout the study period, mean relative tumor volumes are smaller in mice given CYC-116 at either dose than in vehicle-treated mice. At 100 mg/kg po q.d., the growth reduction is statistically significant on days 6 and 9[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay
Prepare CYC-116 in DMSO and dilute in cell medium[1].
Animal Administration[1]
Mice: Implant mice intraperitoneally with P388/0 cells and treat with CYC-116. Measure antitumor activity as the increase in lifespan of treated animals relative to the vehicle control group[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. Sci Transl Med 2018 Jul 18;10(450):eaaq1093.
LIG1 Loss in TP53-mutant Triple Negative Breast Cancer Rewires DNA Repair and Confers Sensitivity to PARP-ATR Inhibitor Combinations. Mol Cancer Ther 2026 Jul 15:10.1158/1535-7163.MCT-26-0182. PMID: 42456172
Ginsenoside Rc Modulates SIRT6-NRF2 Interaction to Alleviate Alcoholic Liver Disease. J Agric Food Chem 2022 Nov 9;70(44):14220-14234. PMID: 36300841
Brefeldin A inhibits colorectal cancer growth by triggering Bip/Akt-regulated autophagy. FASEB J 2019 Apr;33(4):5520-5534.
University of Washington. 2025.
