BDP-13176 Fascin-1 Inhibitor

Fascin has a critical role in cancer cell metastasis by promoting cell migration and invasion. BDP-13176 has a potent affinity to Fascin-1, and is capable of inhibiting the binding of Fascin-1 to filamentous actin.

Contributors

Inventor Institute
Laura Machesky Cancer Research UK, Glasgow: The Beatson Institute
Cat. #: 160596
Tool sub type: Inhibitor
Research Fields: Cancer
Purpose: Inhibitor
Alternate name: FSCN1, Fascin1, Fascin, Fascin actin binding protein
Product 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.
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
Molecular weight: 497
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
Primary target: Fascin-1
Shipping conditions: Dry Ice
References:

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

Related Tools for Small molecules

Cat. # Tool Name
151712 CDK7 inhibitor BS-181 Small Molecule (Tool Compound) Key Info View Tool
152544 Protein Kinase D inhibitor CRT5 (CRT0066051) Small Molecule (Tool Compound) Key Info View Tool
152625 Mps1 inhibitor CCT251455 Small Molecule (Tool Compound) Key Info View Tool
152786 Nucleolar Luminophore Ag-1 Small Molecule (Tool Compound) Key Info View Tool
152788 Phosphatidylinositol-4-phosphate 5-kinase inhibitor PIP5K Small Molecule (Collaborative Toolkit) Key Info View Tool

Tool enquiry

Please ensure you use your organisation email address rather than personal where possible, as this helps us locate your organisation in our system faster.

Please note we may take up to three days to respond to your enquiry.

CancerTools.org uses the contact information provided to respond to you about our research tools and service. For more information please review our privacy policy.