Biological Activity
Raf kinase and VEGFR-2 inhibitor. Inhibits c-Raf, wild type B-Raf and mutant B-Raf (V600E). Cytotoxic in certain melanoma cells lines. Effects enhanced by protein kinase D3 inhibition, preventing reactivation of MAPK signaling and increasing caspase activity. Orally bioavailable.
Technical Data
| M. Wt | 518.41 |
| Formula | C24H16F6N6O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 927880-90-8 |
| PubChem ID | 11656518 |
| InChI Key | YABJJWZLRMPFSI-UHFFFAOYSA-N |
| Smiles | CN1C(NC2=CC=C(C=C2)C(F)(F)F)=NC3=CC(OC4=CC=NC(C5=NC=C(C(F)(F)F)N5)=C4)=CC=C13 |
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 | 51.84 | 100 | |
| ethanol | 10.37 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 518.41. 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 | 1.93 mL | 9.64 mL | 19.29 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.86 mL |
| 10 mM | 0.19 mL | 0.96 mL | 1.93 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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References
References are publications that support the products' biological activity.
Chen et al (2011) Protein kinase D3 sensitizes RAF inhibitor RAF265 in melanoma cells by preventing reactivation of MAPK signaling. Cancer Res. 71 4280 PMID: 21527556
Keywords: RAF 265, supplier, RAF265, Raf, kinases, inhibitors, inhibits, B-Raf, c-Raf, VEGFR2, vascular, endothelial, growth, factor, cytotoxic, MAPK, CHIR, 265, Raf, Kinase, VEGFR, Raf, Kinase, Tocris Bioscience
