BDP-13176 Fascin-1 Inhibitor

Tool Details

*FOR RESEARCH USE ONLY (for other uses, please contact the licensing team)

• 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.