AZ PFKFB3 26

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Cat.No. 5675 - AZ PFKFB3 26 | C24H26N4O2 | CAS No. 1704740-52-2
Description: Potent and selective PFKFB3 inhibitor
Chemical Name: (2S)-N-[4-[[3-Cyano-1-(2-methylpropyl)-1H-indol-5-yl]oxy]phenyl]-2-pyrrolidinecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent and selective PFKFB3 inhibitor (IC50 = 0.023 μM). Selective for PFKFB3 over PFKFB2 and PFKFB1 isoforms (IC50 values are 0.382 μM and 2.06 μM, respectively). Reduces levels of fructose-1,6-bisphosphate in A549 cells (IC50 = 0.343 μM). Exhibits no significant inhibition of other kinases.

Technical Data

M. Wt 402.49
Formula C24H26N4O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1704740-52-2
PubChem ID 118735769
InChI Key OOGHGWKBJXQNEJ-QFIPXVFZSA-N
Smiles N#CC1=CN(CC(C)C)C2=C1C=C(OC3=CC=C(NC([C@H]4NCCC4)=O)C=C3)C=C2

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 40.25 100
ethanol 40.25 100

Preparing Stock Solutions

The following data is based on the product molecular weight 402.49. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.48 mL 12.42 mL 24.85 mL
5 mM 0.5 mL 2.48 mL 4.97 mL
10 mM 0.25 mL 1.24 mL 2.48 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Boyd et al (2015) Structure-based design of potent and selective inhibitors of the metabolic kinase PFKFB3. J.Med.Chem. 58 3611 PMID: 25849762


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Keywords: AZPFKFB326 phosphofructokinase2 PFKFB3 inhibitors inhibits fructose-1,6-bisphosphate kinase cancer PFKFB3

Citations for AZ PFKFB3 26

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Literature in this Area

Cancer

Cancer Research Product Guide

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

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

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

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
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.

Programmed Cell Death

Programmed Cell Death Poster

There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.

Pathways for AZ PFKFB3 26

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