#160596

BDP-13176 Fascin-1 Inhibitor

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Cat. #160596

BDP-13176 Fascin-1 Inhibitor

Cat. #: 160596

Sub-type: Inhibitor

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Contributor

Inventor: Laura Machesky

Institute: Cancer Research UK, Glasgow: The Beatson Institute

Tool Details
Handling
Target Details
References

Tool Details

*FOR RESEARCH USE ONLY

  • Tool name: BDP-13176 Fascin-1 Inhibitor
  • Alternate name: FSCN1, Fascin1, Fascin, Fascin actin binding protein
  • Research fields: Cancer
  • Molecular formula: 5-(3,4-dichlorobenzyl)-4-oxo-1-(piperidin-4-yl)-N-(pyridin-4-yl)-4,5-dihydro-1H-pyrazolo[4,3-c]pyridine-7-carboxamide
  • Chemical name: 5-(3,4-dichlorobenzyl)-4-oxo-1-(piperidin-4-yl)-N-(pyridin-4-yl)-4,5-dihydro-1H-pyrazolo[4,3-c]pyridine-7-carboxamide
  • Tool sub type: Inhibitor
  • Primary target: Fascin-1
  • Description: Fascin is an actin binding and bundling protein that is not expressed in normal epithelial tissues but overexpressed in a variety of invasive epithelial tumors. It has a critical role in cancer cell metastasis by promoting cell migration and invasion. BDP-13176 is a has potent affinity to Fascin-1, and is capable of inhibiting the binding of Fascin-1 to filamentous actin.
  • Purpose: Inhibitor
  • Molecular weight: 497
  • Additional notes: For detailed technical information, please see the manuscript and supplimentary information on Francis et al., 2019. PMID: 30773430 SPR Kd (ÂľM): 0.08 Ligand efficiency: 0.29 Inhibition of actin bundling IC50 (ÂľM): 0.24 Turbidimetric solubility midpoint (ÂľM): 65 logD7.4: 1.8 Molecular weight (Da): 497 Caco-2 permeability A-B Papp (10-6 cm/s): 0.15 Efflux ratio: 37.8 Microsomal CLint (ÂľL/min/mg protein) Mouse: 11.8 Human: 6.4 CYP450 IC50 (ÂľM) CYP3A4: 7 CYP2D6: 1.6 CYP2C19: 22 CYP2C9: 5.9 hERG IC50 (ÂľM): >25

Handling

  • Purity: 497 g/mol
  • Shipping conditions: Dry Ice

Target Details

  • Primary target: Fascin-1
  • Ic50: 0.24 ± 0.01 ÂľM

References

  • Francis et al. 2019. Bioorg Med Chem Lett. 29(8):1023-1029. PMID: 30773430.