SMALL MOLECULES
Contributor Information
- Name Laura Machesky
- Institute Cancer Research UK, Glasgow: The Beatson Institute
Tool Details
- Tool name: BDP-13176 Fascin-1 Inhibitor
- Alternate names: FSCN1, Fascin1, Fascin, Fascin actin binding protein
- 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 type: Small molecules
- Tool sub-type: Inhibitor
- Purpose: Inhibitor
- Molecular weight of the target: 497
- 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.
- Research area: Cancer
- IC50: 0.24âŻÂąâŻ0.01 ÂľM
- 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
- For Research Use Only
Target Details
- Target molecular weight: 497
- Primary target: Fascin-1
Application Details
Handling
- Purity: 497 g/mol
- Shipping conditions: Dry Ice
Documentation
- Available on request
Related Tools
References
- • Francis et al. 2019. Bioorg Med Chem Lett. 29(8):1023-1029. PMID: 30773430.
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