2. Cell Cycle/DNA Damage
  3. Polo-like Kinase (PLK)
  4. Centrinone

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

For research use only. We do not sell to patients.

Centrinone Chemical Structure

Centrinone Chemical Structure

CAS No. : 1798871-30-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 201 In-stock
Solution
10 mM * 1 mL in DMSO USD 201 In-stock
Solid
1 mg USD 68 In-stock
5 mg USD 144 In-stock
10 mg USD 240 In-stock
50 mg USD 1080 In-stock
100 mg USD 2040 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of Centrinone:

Centrinone Related Antibodies

Top Publications Citing Use of Products

View All Polo-like Kinase (PLK) Isoform Specific Products:

View All Isoforms
PLK1 PLK2 PLK3 PLK4

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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]
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]
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]
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
Molecular Weight

633.65

Formula

C26H25F2N7O6S2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

FC(C([N+]([O-])=O)=CC=C1)=C1CS(C2=CC(F)=C(SC3=NC(NC4=NNC(C)=C4)=C(OC)C(N5CCOCC5)=N3)C=C2)(=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (48.92 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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: ≥ 2.5 mg/mL (3.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (3.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.16%

SDS (393 KB)

COA (250 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Purified 6xHis-tagged human Plk4 kinase domain is in 20 mM Tris pH 7.5, 100 mM NaCl, 10% glycerol, 1 mM DTT. 2X reaction buffer consists of 50 mM HEPES pH 8.5, 20 mM MgCl2, 1 mM DTT, 0.2 mg/mL BSA, 16 μM ATP, and 200 μM A-A11 substrate. The Plk4 concentration in the final reaction is 2.5-10 nM with a final pH of 8.0. Inhibitors (Centrinone) array in dose response are added from DMSO stocks. Reactions are allowed to proceed for 4-16 hours at 25°C. Detection is performed using ADP-Glo reagent. Luminescence is measured on an plate reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

For each condition, cells are seeded in triplicate into 6-well plates at 50,000 cells/well. 125 nM Centrinone (LCR-263) is added to HeLa cells or 300 nM is added to NIH/3T3 cells. At 24-hour intervals, 3 wells are harvested per condition. Cell counting is performed using a TC10 automated cell counter[1].

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

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5782 mL 7.8908 mL 15.7816 mL 39.4540 mL
5 mM 0.3156 mL 1.5782 mL 3.1563 mL 7.8908 mL
10 mM 0.1578 mL 0.7891 mL 1.5782 mL 3.9454 mL
15 mM 0.1052 mL 0.5261 mL 1.0521 mL 2.6303 mL
20 mM 0.0789 mL 0.3945 mL 0.7891 mL 1.9727 mL
25 mM 0.0631 mL 0.3156 mL 0.6313 mL 1.5782 mL
30 mM 0.0526 mL 0.2630 mL 0.5261 mL 1.3151 mL
40 mM 0.0395 mL 0.1973 mL 0.3945 mL 0.9863 mL
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Centrinone Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Centrinone1798871-30-3LCR-263LCR263LCR 263Polo-like Kinase (PLK)Inhibitorinhibitorinhibit

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