Centrinone B

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Cat.No. 5690 - Centrinone B | C27H27F2N7O5S2 | CAS No. 1798871-31-4
Description: High affinity and selective PLK4 inhibitor
Alternative Names: LCR 323
Chemical Name: 2-[[2-Fluoro-4-[[(2-fluoro-3-nitrophenyl)methyl]sulfonyl]phenyl]thio]-5-methoxy-N-(5-methyl-1H-pyrazol-3-yl)-6-(1-piperidinyl)-4-pyrimidinamine
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

Biological Activity

High affinity and selective PLK4 inhibitor (Ki = 0.6 nM). Exhibits >2000-fold selectivity for PLK4 over Aurora A and Aurora B. Depletes centriole and centrosome levels in vitro. Induces cell cycle arrest in normal human cell lines in a p53-dependent manner.

Licensing Information

Sold with the permission of the Ludwig Institute for Cancer Research Ltd

Technical Data

M. Wt 631.67
Formula C27H27F2N7O5S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1798871-31-4
PubChem ID 118704753
InChI Key UPZNTUYHCRQOIQ-UHFFFAOYSA-N
Smiles FC1=C([N+]([O-])=O)C=CC=C1CS(C2=CC=C(SC3=NC(N4CCCCC4)=C(OC)C(NC5=NNC(C)=C5)=N3)C(F)=C2)(=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 31.58 50

Preparing Stock Solutions

The following data is based on the product molecular weight 631.67. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.58 mL 7.92 mL 15.83 mL
5 mM 0.32 mL 1.58 mL 3.17 mL
10 mM 0.16 mL 0.79 mL 1.58 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Wong et al (2015) Reversible centriole depletion with an inhibitor of Polo-like kinase 4. Science 348 1155 PMID: 25931445


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Keywords: Centrinone B, supplier, LCR323, high, affinity, selective, PLK4, inhibitors, inhibits, centriole, centrosome, LCR, 323, Polo-like, Kinase, Mitosis, Polo-like, Kinase, Tocris Bioscience

1 Citation for Centrinone B

Citations are publications that use Tocris products. Selected citations for Centrinone B include:

Chen et al (2017) Human microcephaly protein RTTN interacts with STIL and is required to build full-length centrioles. Nat Commun 8 247 PMID: 28811500


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Literature in this Area

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

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Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.