Biological Activity
Selective ARF6 inhibitor (IC50 = 1.0 μM). Selective for ARF6 over other ARF family members and small GTPases. Inhibits ARF6 activation in uveal melanoma cells in vitro and blocks downstream signaling pathways of oncogenic GNAQ. Reduces tumorigenesis in mouse model of uveal melanoma.
Technical Data
| M. Wt | 456.88 |
| Formula | C25H17ClN4O3 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 419547-11-8 |
| PubChem ID | 2257249 |
| InChI Key | WHYGBVWGARJOCS-UHFFFAOYSA-N |
| Smiles | ClC1=CC=C(C2=C3NC(C4=CC=C([N+]([O-])=O)C=C4)=CC(N3N=C2CC5=CC=CC=C5)=O)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.69 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 456.88. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.19 mL | 10.94 mL | 21.89 mL |
| 5 mM | 0.44 mL | 2.19 mL | 4.38 mL |
| 10 mM | 0.22 mL | 1.09 mL | 2.19 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Yoo et al (2016) ARF6 is an actionable node that orchestrates oncogenic GNAQ signaling in uveal melanoma. Cancer Cell. 29 889 PMID: 27265506
Keywords: NAV 2729, supplier, NAV2729, small, G, proteins, Gαq, GTPases, inhibitors, inhibits, selective, ARF6, GNAQ, G, Proteins, (Small), GTPase, GTPase, Tocris Bioscience
