Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.
 
> CYC-116 [693228-63-6]

CYC-116 [693228-63-6]

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Referência HY-10558-10mg

Tamanho : 10mg

Marca : MedChemExpress

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Description

CYC-116 is a potent aurora A and aurora B inhibitor with Kis of 8 and 9 nM, respectively.

IC50 & Target[1]

Aurora A

8 nM (Ki)

Aurora B

9.2 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
A2780 IC50
170 nM
Compound: 18, CYC-116
Cytotoxicity against human A2780 cells after 96 hrs by MTT assay
Cytotoxicity against human A2780 cells after 96 hrs by MTT assay
[PMID: 20462263]
A549 IC50
0.48 μM
Compound: 18, CYC-116
Inhibition of Aurora kinase in human A549 cells assessed as concentration required for half-maximal inhibition of histone H3 serine-10 phosphorylation after 7 hrs immunofluorescence microscopy
Inhibition of Aurora kinase in human A549 cells assessed as concentration required for half-maximal inhibition of histone H3 serine-10 phosphorylation after 7 hrs immunofluorescence microscopy
[PMID: 20462263]
BXPC-3 IC50
1.626 μM
Compound: 18, CYC-116
Cytotoxicity against human BxPC3 cells after 96 hrs by MTT assay
Cytotoxicity against human BxPC3 cells after 96 hrs by MTT assay
[PMID: 20462263]
CCRF-CEM IC50
0.471 μM
Compound: 18, CYC-116
Cytotoxicity against human CCRF-CEM cells after 96 hrs by MTT assay
Cytotoxicity against human CCRF-CEM cells after 96 hrs by MTT assay
[PMID: 20462263]
COLO 205 IC50
0.241 μM
Compound: 18, CYC-116
Cytotoxicity against human COLO205 cells after 96 hrs by MTT assay
Cytotoxicity against human COLO205 cells after 96 hrs by MTT assay
[PMID: 20462263]
HCT-116 IC50
0.34 μM
Compound: 18, CYC-116
Cytotoxicity against human HCT116 cells after 96 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 96 hrs by MTT assay
[PMID: 20462263]
HeLa IC50
0.59 μM
Compound: 18, CYC-116
Cytotoxicity against human HeLa cells after 96 hrs by MTT assay
Cytotoxicity against human HeLa cells after 96 hrs by MTT assay
[PMID: 20462263]
HL-60 IC50
0.372 μM
Compound: 18, CYC-116
Cytotoxicity against human HL60 cells after 96 hrs by MTT assay
Cytotoxicity against human HL60 cells after 96 hrs by MTT assay
[PMID: 20462263]
HT-29 IC50
0.725 μM
Compound: 18, CYC-116
Cytotoxicity against human HT-29 cells after 96 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 96 hrs by MTT assay
[PMID: 20462263]
HuP-T4 IC50
0.775 μM
Compound: 18, CYC-116
Cytotoxicity against human HUPT4 cells after 96 hrs by MTT assay
Cytotoxicity against human HUPT4 cells after 96 hrs by MTT assay
[PMID: 20462263]
K562 IC50
1.375 μM
Compound: 18, CYC-116
Cytotoxicity against human K562 cells after 96 hrs by MTT assay
Cytotoxicity against human K562 cells after 96 hrs by MTT assay
[PMID: 20462263]
MCF7 IC50
0.599 μM
Compound: 18, CYC-116
Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay
[PMID: 20462263]
MES-SA IC50
0.09 μM
Compound: 18, CYC-116
Cytotoxicity against human MESSA cells after 96 hrs by MTT assay
Cytotoxicity against human MESSA cells after 96 hrs by MTT assay
[PMID: 20462263]
MIA PaCa-2 IC50
278 nM
Compound: 18, CYC-116
Cytotoxicity against human MIAPaCa2 cells after 96 hrs by MTT assay
Cytotoxicity against human MIAPaCa2 cells after 96 hrs by MTT assay
[PMID: 20462263]
MV4-11 IC50
0.034 μM
Compound: 18, CYC-116
Cytotoxicity against human MV4-11 cells after 96 hrs by MTT assay
Cytotoxicity against human MV4-11 cells after 96 hrs by MTT assay
[PMID: 20462263]
NCI-H460 IC50
0.681 μM
Compound: 18, CYC-116
Cytotoxicity against human NCI-H460 cells after 96 hrs by MTT assay
Cytotoxicity against human NCI-H460 cells after 96 hrs by MTT assay
[PMID: 20462263]
SAOS-2 IC50
0.11 μM
Compound: 18, CYC-116
Cytotoxicity against human Saos2 cells after 96 hrs by MTT assay
Cytotoxicity against human Saos2 cells after 96 hrs by MTT assay
[PMID: 20462263]
In Vitro

CYC-116 also inhibits VEGFR2, Src, Lck AND FLT3 with with Kis of 44, 82, 280, 44 nM, respectively. CYC-116 may have broad-spectrum antitumor activity. 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. Treatment with 1.25 μM CYC-116 for 7 h results in complete inhibition of histone H3 phosphorylation in HeLa cell lysates[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CYC-116 Related Antibodies

Solvant et solubilité
In Vitro: 

DMSO : 15 mg/mL (40.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7140 mL 13.5700 mL 27.1400 mL
5 mM 0.5428 mL 2.7140 mL 5.4280 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 1.5 mg/mL (4.07 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.5 mg/mL (4.07 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Pureté et documentation
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