BDP-13176 Fascin-1 Inhibitor
Invented by Prof Laura Machesky from Cancer Research UK Glasgow: The Beatson Institute
Invented at Cancer Research UK Glasgow: The Beatson Institute
- Datasheet
- References (1)
- Inventor Info
Info
| Catalogue Number | 160596 |
| Antigen/Gene or Protein Targets | Fascin-1 |
| Synonyms | FSCN1, Fascin1, Fascin, Fascin actin binding protein |
| Type | Inhibitor |
| Relevance | 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. |
| On Target IC50 | 0.24 ± 0.01 µM |
| 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 |
| Molecular Weight (g/mol) | 497 |
| Research Area | Cancer |
| Notes |
For detailed technical information, please see the manuscript and supplimentary information on Francis et al., 2019. PMID: 30773430 SPR Kd (µM): 0.08 Ligand efficiency: 0.29 Inhibition of actin bundling IC50 (µM): 0.24 Turbidimetric solubility midpoint (µM): 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 (µL/min/mg protein) Mouse: 11.8 Human: 6.4 CYP450 IC50 (µM) CYP3A4: 7 CYP2D6: 1.6 CYP2C19: 22 CYP2C9: 5.9 hERG IC50 (µM): >25 |
