SBE 13 hydrochloride

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Cat.No. 4292 - SBE 13 hydrochloride | C24H27ClN2O4.HCl | CAS No. 1052532-15-6
Description: Potent and selective PLK1 inhibitor
Chemical Name: N-[[4-[(6-Chloro-3-pyridinyl)methoxy]-3-methoxyphenyl]methyl]-3,4-dimethoxybenzeneethanamine hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively). Exhibits no effect on Aurora kinase A activity. Binds and stabilizes the inactive form of PLK1. Delays cell cycle progression, reduces cell proliferation and induces apoptosis in a range of human cancer cell lines. Transiently arrests cells cycle at G0/G1 in primary cells.

Compound Libraries

SBE 13 hydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 479.4
Formula C24H27ClN2O4.HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 1052532-15-6
PubChem ID 11948807
InChI Key QBGSVDJLQQXEGG-UHFFFAOYSA-N
Smiles ClC(N=C3)=CC=C3COC1=C(OC)C=C(CNCCC2=CC(OC)=C(OC)C=C2)C=C1.Cl

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 47.94 100
water 4.79 10 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 479.4. 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 2.09 mL 10.43 mL 20.86 mL
5 mM 0.42 mL 2.09 mL 4.17 mL
10 mM 0.21 mL 1.04 mL 2.09 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the biological activity of the product.

Eckerdt (2010) Freezing Polo in its sleep: targeting the inactive conformation of Polo-like kinase 1 in cancer cells. Cell Cycle 9 862 PMID: 20348843

Keppner et al (2010) Biological impact of freezing Plk1 in its inactive conformation in cancer cells. Cell Cycle 9 761 PMID: 20139717

Liu (2010) SBE13 joins the family of Polo-like kinase 1 (Plk1) inhibitors. Cell Cycle 9 445 PMID: 20130451

Keppner et al (2011) Fate of primary cells at the G1/S boundary after Polo-like kinase 1 inhibition by SBE13. Cell Cycle 10 708 PMID: 21301227

Keppner et al (2009) Identification and validation of a potent type II inhibitor of inactive polo-like kinase 1. ChemMedChem 4 1806 PMID: 19746360


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Citations for SBE 13 hydrochloride

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Literature in this Area

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Cancer Research Product Guide

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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.