CYC116 |
| カタログ番号GC15106 |
強力なオーロラキナーゼ阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 693228-63-6
Sample solution is provided at 25 µL, 10mM.
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IC50: 44 and 19 nM respectively for Aurora A and B in cancer cells
Ki: 8.0 and 9.2 nM for aurora A and B, respectively
The aurora kinases are a family of serine-threonine kinases that interact with components of the mitotic apparatus and that regulate aspects of centrosome maturation, bipolar spindle assembly, chromosome segregation, and cytokinesis. CYC116 has been discoverd as a novel N-phenyl-4-(thiazol-5-yl) pyrimidin-2-amine aurora kinase inhibitor.
In vitro: The anticancer effects of CYC116 were shown to emanate from cell death following mitotic failure and increased polyploidy as a consequence of cellular inhibition of aurora A and B kinases. Moreover, CYC116 was also assessed against other kinases [1].
In vivo: Preliminary in vivo assessment showed that CYC116 was orally bioavailable and possessed anticancer activity. The mean relative tumor volumes of mice receiving CYC116 at both dose levels were less than those of vehicle-treated mice for the duration of the study period [1].
Clinical trials: CYC116 is currently undergoing evaluation in Phase I clinical trials.
Reference:
[1] Wang S, Midgley CA, Scaërou F, Grabarek JB, Griffiths G, Jackson W, Kontopidis G, McClue SJ, McInnes C, Meades C, Mezna M, Plater A, Stuart I, Thomas MP, Wood G, Clarke RG, Blake DG, Zheleva DI, Lane DP, Jackson RC, Glover DM, Fischer PM. Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J Med Chem. 2010;53(11):4367-78.
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Kinase experiment: |
Aurora A kinase assays are performed using a 25 μL reaction volume (25 mM β-glycerophosphate, 20 mM Tris/HCl, pH 7.5, 5 mM EGTA, 1 mM DTT, 1 mM Na3VO4, 10 μg of kemptide (peptide substrate)), and recombinant aurora A kinase is diluted in 20 mM Tris/HCl, pH 8, containing 0.5 mg/mL BSA, 2.5% glycerol, and 0.006% Brij-35. Reactions are started by the addition of 5 μL Mg/ATP mix (15 mM MgCl4, 100 μM ATP, with 18.5 kBq γ-32P-ATP per well) and incubated at 30°C for 30 min before terminating by the addition of 25 μL of 75 mM H3PO4. Aurora B kinase assays are performed as for aurora A except that prior to use, aurora B is activated in a separate reaction at 30°C for 60 min with inner centromeres protein[1]. |
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Cell experiment: |
CYC-116 is prepared in DMSO and diluted in cell medium[1]. |
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Animal experiment: |
Mice: Mice implanted intraperitoneally with P388/0 cells are treated with CYC-116, and the antitumor activity is measured as an increase in lifespan of the treated animals versus the vehicle control group[1]. |
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References: [1]. Wang S, et al. Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J Med Chem. 2010 Jun 10;53(11):4367-78. |
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| Cas No. | 693228-63-6 | SDF | |
| Chemical Name | 4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine | ||
| Canonical SMILES | CC1=C(SC(=N1)N)C2=NC(=NC=C2)NC3=CC=C(C=C3)N4CCOCC4 | ||
| Formula | C18H20N6OS | M.Wt | 368.46 |
| 溶解度 | ≥ 18.4 mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.714 mL | 13.57 mL | 27.14 mL |
| 5 mM | 0.5428 mL | 2.714 mL | 5.428 mL |
| 10 mM | 0.2714 mL | 1.357 mL | 2.714 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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