Centrinone (Synonyms: LCR-263)

Name: Centrinone
Brand: MedChemExpress
SKU: HY-18682
Rating: 5.0 (32 reviews)

Cat. No.: HY-18682 Purity: 98.28%: Data Sheet
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Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a K_i of 0.16 nM.

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

CAS No. : 1798871-30-3

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 32 publication(s) in Google Scholar

Other Forms of Centrinone:

Centrinone-B In-stock

32 Publications Citing Use of MCE Centrinone

Cell Imaging/Staining

Bio/Physico-chemical Assay

: Centrinone purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Oct 15;15(1):8890. [Abstract]; Centrinone (25-100 nM; 3 d) reduced centriole count in pro B cell cultures in a dose and time-dependent manner in all genotypes alike.

: Centrinone purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Oct 15;15(1):8890. [Abstract]; Centriole depletion assessed by IF with γ-Tubulin, CP110 antibodies, and Hoechst staining in iGC B cells cultured on feeder cells with IL-4 for 4 days ± Centrinone (125-200 nM).

: Centrinone purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Oct 15;15(1):8890. [Abstract]; The bar graph showed the percentage of cells staining positive for the DNA marker TO-PRO3 among pro B cells cultured with Centrinone (125 nM; 3 d).

: Centrinone purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2019 Dec;21(12):1544-1552. [Abstract]; Images from videos of Centrin 2-GFP-expressing Deup1^-/- ependymal cells transiently treated with Centrinone (0.6 μM) to deplete the preexisting centrioles.

: Centrinone purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2019 Dec;21(12):1544-1552. [Abstract]; Correlative light and electron microscopy of Centrin 2-GFP-expressing Deup1^-/- ependymal cells treated with Centrinone (0.6 μM) to deplete the parent centrioles.

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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 K_i 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.

Molecular Weight

633.65

Formula

C₂₆H₂₅F₂N₇O₆S₂

CAS No.

1798871-30-3

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 : 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
10 mM	0.1578 mL	0.7891 mL	1.5782 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 98.28%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (250 KB) HNMR (139 KB) RP-HPLC (168 KB) LCMS (105 KB)

Handling Instructions (2659 KB)

References

[1]. Wong YL. et al. Cell biology. Reversible centriole depletion with an inhibitor of Polo-like kinase 4. Science. 2015 Jun 5;348(6239):1155-60. [Content Brief]

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	[1]. Wong YL. et al. Cell biology. Reversible centriole depletion with an inhibitor of Polo-like kinase 4. Science. 2015 Jun 5;348(6239):1155-60. [Content Brief]

Complete Stock Solution Preparation Table

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
	50 mM	0.0316 mL	0.1578 mL	0.3156 mL	0.7891 mL
	60 mM	0.0263 mL	0.1315 mL	0.2630 mL	0.6576 mL
	80 mM	0.0197 mL	0.0986 mL	0.1973 mL	0.4932 mL
	100 mM	0.0158 mL	0.0789 mL	0.1578 mL	0.3945 mL

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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Centrinone (Synonyms: LCR-263)

Customer Review

Other Forms of Centrinone:

Centrinone Related Antibodies

32 Publications Citing Use of MCE Centrinone

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

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

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Centrinone Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Centrinone Related Classifications

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