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> Centrinone [1798871-30-3]

Centrinone [1798871-30-3]

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Referência HY-18682-1mL

Tamanho : 10mM/1mL

Marca : MedChemExpress

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Description

Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM.

IC50 & Target[1]

PLK4

0.16 nM (Ki)

PLK4 (G95L)

68.57 nM (Ki)

Aurora A

171 nM (Ki)

Aurora B

436.76 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
BT-474 IC50
10.52 μM
Compound: 3
Antiproliferative activity against human BT-474 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
Antiproliferative activity against human BT-474 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
[PMID: 35576702]
BT-474 IC50
10.52 μM
Compound: LCR-263
Antiproliferative activity against human BT-474 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
Antiproliferative activity against human BT-474 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
[PMID: 37731702]
BT-474 IC50
11.02 μM
Compound: 5
Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay
Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay
[PMID: 36063666]
HUVEC IC50
5.6 μM
Compound: 5
Cytotoxicity against human HUVEC assessed as inhibition of cell growth incubated for 5 days by MTT assay
Cytotoxicity against human HUVEC assessed as inhibition of cell growth incubated for 5 days by MTT assay
[PMID: 36063666]
K562 IC50
0.35 μM
Compound: 3; LCR-263
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 5 days
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 5 days
[PMID: 36734825]
L02 IC50
7.26 μM
Compound: 5
Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay
Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay
[PMID: 36063666]
MCF7 IC50
1.62 μM
Compound: 3; LCR-263
Antiproliferative activity against human MCF7 cells incubated for 5 days by CCK-8 assay
Antiproliferative activity against human MCF7 cells incubated for 5 days by CCK-8 assay
[PMID: 37279162]
MCF7 IC50
2.05 μM
Compound: 5
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay
[PMID: 36063666]
MCF7 IC50
2.27 μM
Compound: 3
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
[PMID: 35576702]
MCF7 IC50
2.27 μM
Compound: LCR-263
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
[PMID: 37731702]
MDA-MB-231 IC50
10.22 μM
Compound: 5
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 5 days by MTT assay
[PMID: 36063666]
MDA-MB-231 IC50
8.69 μM
Compound: 3
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
[PMID: 35576702]
MDA-MB-231 IC50
8.69 μM
Compound: LCR-263
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
[PMID: 37731702]
In Vitro

Centrinone (LCR-263) exhibits more than 1000-fold selectivity for Plk4 over Aurora A/B and does not affect cellular Aurora A or B substrate phosphorylation at concentrations that deplete centrosomes. Centrinone (LCR-263) treatment of HeLa human cervical carcinoma cells leads to a progressive reduction in foci containing centriolar and pericentriolar material markers at each round of cell division, until most cells lack centrioles and centrosomes. Treatment with Centrinone (LCR-263) reduces centriole number in multiciliated Xenopus epithelial cells, which indicates that Plk4 also controls centriole amplification in differentiated cells. Centrinone (LCR-263) treatment causes centrosome depletion in human and other vertebrate cells. Centrosome loss irreversibly arrests normal cells in a senescence-like G1 state by a p53-dependent mechanism that is independent of DNA damage, stress, Hippo signaling, extends mitotic duration, or segregation errors[1].

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

Centrinone Related Antibodies

Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (157.82 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 1.5782 mL 7.8908 mL 15.7816 mL
5 mM 0.3156 mL 1.5782 mL 3.1563 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: ≥ 5 mg/mL (7.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

    Solubility: ≥ 5 mg/mL (7.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Pureté et documentation
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