Reagenzien und Instrumente für die Immunologie Zellbiologie und Molekularbiologie
 
> CCT 137690 [1095382-05-0]

CCT 137690 [1095382-05-0]

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Katalog-Nummer HY-10804-5mg

Size : 5mg

Marke : MedChemExpress


Beschreibung

CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively.

IC50 & Target[1]

Aurora A

15 nM (IC50)

Aurora B

25 nM (IC50)

Aurora C

19 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
A2780 GI50
0.3 μM
Compound: 71; CCT137690
Growth inhibition of human A2780 cells incubated for 72 hrs by MTT assay
Growth inhibition of human A2780 cells incubated for 72 hrs by MTT assay
[PMID: 28918096]
SW-620 GI50
0.14 μM
Compound: 71; CCT137690
Growth inhibition of human SW620 cells incubated for 72 hrs by MTT assay
Growth inhibition of human SW620 cells incubated for 72 hrs by MTT assay
[PMID: 28918096]
In Vitro

CCT 137690 displays antiproliferative activity in a range of human tumor cell lines, including SW620 colon carcinoma (GI50=0.30 μM) and A2780 ovarian cancer cell line (GI50=0.14 μM). CCT 137690 inhibits in vitro phosphorylation of histone H3. CCT 137690 is a moderate inhibitor of the hERG ion-channel (IC50=3.0 μM)[1]. CCT137690 efficiently inhibits histone H3 and TACC3 phosphorylation (Aurora B and Aurora A substrates, respectively) in HCT116 and HeLa cells. Continuous exposure of tumour cells to the inhibitor causes multipolar spindle formation, chromosome misalignment, polyploidy and apoptosis[2].

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

CCT 137690 Related Antibodies

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 16.67 mg/mL (30.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8133 mL 9.0665 mL 18.1330 mL
5 mM 0.3627 mL 1.8133 mL 3.6266 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: ≥ 1.67 mg/mL (3.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: ≥ 1.67 mg/mL (3.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
Reinheit & Dokumentation
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