Biological Activity
Ras-Net (Elk-3) pathway inhibitor (IC50 = 10 - 20 nM). Indirectly inhibits Net phosphorylation upstream of Erk1/2 activation. Mediates G2-M cell cycle arrest, suppresses growth of multiple cell types (IC50 ~ 2 nM), inhibits angiogenesis and acts as a microtubule depolymerizing agent in vitro.
Technical Data
| M. Wt | 380.87 |
| Formula | C21H21ClN4O |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 729605-21-4 |
| PubChem ID | 10339779 |
| InChI Key | NPHPNBGYPKBDDB-UHFFFAOYSA-N |
| Smiles | CC1=NN(C2=CC=CC=C2)C(C(N3CCN(C4=CC(Cl)=CC=C4)CC3)=O)=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 | 38.09 | 100 | |
| ethanol | 19.04 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 380.87. 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 | 2.63 mL | 13.13 mL | 26.26 mL |
| 5 mM | 0.53 mL | 2.63 mL | 5.25 mL |
| 10 mM | 0.26 mL | 1.31 mL | 2.63 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Wasylyk et al (2008) Inhibition of the Ras-Net (Elk-3) pathway by a novel pyrazole that affects microtubules. Cancer Res. 68 1275 PMID: 18316589
Keywords: XRP44X, supplier, Ras-Net, pathway, inhibitors, inhibits, Antiangiogenics, microtubule, depolymerization, depolymerisation, agent, MAPK, Signaling, Signalling, G, Proteins, Small, Mitogen-Activated, Protein, Kinases, Tau, Tubulin, Microtubules, G, Proteins, (Small), Other, MAPK, Antiangiogenics, Mitosis, Other, MAPK, Tocris Bioscience
