製品番号: HY-18682

Centrinone

Name: Centrinone
Brand: MedChemExpress
SKU: HY-18682
Price: 68.00 USD
Availability: InStock
Rating: 5 (35 reviews)

(別名: LCR-263)

35 Cited Publications

カスタマーレビュー

Based on 35 publication(s) in Google Scholar

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

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純度 : 98.30%
CAS 番号: 1798871-30-3
分子式: C₂₆H₂₅F₂N₇O₆S₂
分子量:633.65

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Centrinone 構造式

CAS 番号: 1798871-30-3

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数量

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
化学情報
Publications (35)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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)

Polo-like Kinase (PLK) アイソフォーム固有の製品をすべて表示 :

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]
KU812 cell line	IC₅₀	1.06 μM Compound: 3; LCR-263	Antiproliferative activity against human KU812 cells assessed as inhibition of cell growth incubated for 5 days Antiproliferative activity against human KU812 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]

体外実験

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. .

化学情報

CAS 番号 1798871-30-3
性状 Solid
分子量 633.65
分子式 C₂₆H₂₅F₂N₇O₆S₂
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
別名

LCR-263
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (35)

All Cell Imaging/StainingBio/Physico-chemical AssayIF

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Journal Impact Factor

Nat Cell Biol

Massive centriole production can occur in the absence of deuterosomes in multiciliated cells. [Abstract]

2019 Dec;21(12):1544-1552. PMID: 31792378

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.
Nat Commun

Centrioles are frequently amplified in early B cell development but dispensable for humoral immunity. [Abstract]

2024 Oct 15;15(1):8890. PMID: 39406735

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).
Nat Commun

Self-organization of Plk4 regulates symmetry breaking in centriole duplication. [Abstract]

2019 Apr 18;10(1):1810. PMID: 31000710
Sci Adv

Influenza A virus subverts the LC3-pericentrin dynein adaptor complex for host cytoplasm entry. [Abstract]

2025 Jun 13;11(24):eadu7602. PMID: 40498831
Sci Adv

Rapid and sustained degradation of the essential centrosome protein CEP192 in live mice using the AID2 system. [Abstract]

2025 Feb 28;11(9):eadq2339. PMID: 40020058
EMBO J

Aurora A regulates the material property of spindle poles to orchestrate nuclear organization at mitotic exit. [Abstract]

2025 Sep 12. PMID: 40940421
EMBO J

Extra centrosomes induce PIDD1-mediated inflammation and immunosurveillance. [Abstract]

2023 Oct 16;42(20):e113510. PMID: 37530438
EMBO J

NuMA assemblies organize microtubule asters to establish spindle bipolarity in acentrosomal human cells. [Abstract]

2020 Jan 15;39(2):e102378. PMID: 31782546
Curr Biol

Microtubule nucleation from the fibrous corona by LIC1-pericentrin promotes chromosome congression. [Abstract]

2023 Mar 13;33(5):912-925.e6. PMID: 36720222
J Med Chem

Discovery of CZS-241: A Potent, Selective, and Orally Available Polo-Like Kinase 4 Inhibitor for the Treatment of Chronic Myeloid Leukemia. [Abstract]

2023 Feb 23;66(4):2396-2421. PMID: 36734825
Cancer Cell Int

2026 Jun 18. PMID: 42316241
Mol Cancer Ther

2026 Jul 15:10.1158/1535-7163.MCT-26-0182. PMID: 42456172
J Cell Biol

A theory of centriole duplication based on self-organized spatial pattern formation. [Abstract]

2019 Nov 4;218(11):3537-3547. PMID: 31451615
Int J Mol Sci

Centrosome, the Newly Identified Passenger through Tunneling Nanotubes, Increases Binucleation and Proliferation Marker in Receiving Cells. [Abstract]

2021 Sep 7;22(18):9680. PMID: 34575851
Mol Med Rep

MicroRNA‑155‑5p inhibits trophoblast cell proliferation and invasion by disrupting centrosomal function. [Abstract]

2024 May;29(5):85. PMID: 38551159
RSC Med Chem

Design, synthesis, and biological evaluation of novel N-(1 H-indazol-6-yl)benzenesulfonamide derivatives as potent PLK4 inhibitors. [Abstract]

2025 May 13. PMID: 40521341
Mol Oncol

NUAK1 governs centrosome replication in pancreatic cancer via MYPT1/PP1β and GSK3β-dependent regulation of PLK4. [Abstract]

2023 Jul;17(7):1212-1227. PMID: 36975767
Biomedicines

Defect of IL17 Signaling, but Not Centrinone, Inhibits the Development of Psoriasis and Skin Papilloma in Mouse Models. [Abstract]

2022 Aug 15;10(8):1976. PMID: 36009523
BMC Bioinformatics

CenFind: a deep-learning pipeline for efficient centriole detection in microscopy datasets. [Abstract]

2023 Mar 28;24(1):120. PMID: 36977999
Pathol Res Pract

Downregulation of Polo-like kinase 4 induces cell apoptosis and G2/M arrest in acute myeloid leukemia. [Abstract]

2023 Mar:243:154376. PMID: 36821942
J Cancer Res Clin Oncol

Anticancer effects of the PLK4 inhibitors CFI-400945 and centrinone in Ewing's sarcoma cells. [Abstract]

2020 Nov;146(11):2871-2883. PMID: 32770382
J Formos Med Assoc

Roles of centrioles in neural attraction of dental pulp stem cells. [Abstract]

2024 Sep;123(9):934-941. PMID: 38155028
Photochem Photobiol

PLK4 is a potential therapeutic target in nonmelanoma skin cancers: Evidence from molecular and in vivo studies. [Abstract]

2025 Jun 16:10.1111/php.70006. PMID: 40524317
Biol Open

Feedback loops in the Plk4-STIL-HsSAS6 network coordinate site selection for procentriole formation. [Abstract]

2019 Sep 18;8(9):bio047175. PMID: 31533936
University of California, Santa Barbara

2026.
bioRxiv

2025 Sep 18.
bioRxiv

2025 May 21.
bioRxiv

2025 March 06.
bioRxiv

PLK4 inhibition as a strategy to enhance non-small cell lung cancer radiosensitivity. [Abstract]

2025 Feb 23:2025.02.19.638860. PMID: 40027806
bioRxiv

2024 October 01.
biorxiv

2024 Jun 05.
bioRxiv

2024 Feb 15.
University of Zürich

2021 Dec.
Elife

TRIM37 prevents formation of centriolar protein assemblies by regulating Centrobin. [Abstract]

2021 Jan 25:10:e62640. PMID: 33491649
Ruperto Carola University Heidelberg

2019.

溶剤 & 溶解度

体外:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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参考文献

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
	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

Bioz

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Centrinone

35 Cited Publications

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Centrinone

MedChemExpress（MCE）の使用を引用している文献 Centrinone

Polo-like Kinase (PLK) アイソフォーム固有の製品をすべて表示

生物活性