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Biological Activity
PLX-4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf.
Targets
| Target | Value |
|---|---|
| C-Raf-1(Y340D/Y341D) | IC50: 6.7nM |
| B-Raf(V600E) | IC50: 13nM |
| BRK | IC50: 130nM |
| B-Raf | IC50: 160nM |
| FRK | IC50: 1.3μM |
| CSK | IC50: 1.5μM |
| Src | IC50: 1.7μM |
| FAK | IC50: 1.7μM |
| FGFR | IC50: 1.9μM |
| KDR | IC50: 2.3μM |
| HGK | IC50: 2.8μM |
| CSF-1R | IC50: 3.3μM |
| AuroraA | IC50: 3.4μM |
| In vitro (25°C) | DMSO | 81 mg/mL (195.73 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 2% DMSO+50% PEG 300+5% Tween 80+ddH2O | 4 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 24.17 mL | 120.83 mL | 241.66 mL |
| 0.5 mM | 4.83 mL | 24.17 mL | 48.33 mL |
| 1 mM | 2.42 mL | 12.08 mL | 24.17 mL |
| 5 mM | 0.48 mL | 2.42 mL | 4.83 mL |
*The above data is based on the productmolecular weight 413.8. 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.
| Catalog Num | A10002 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 918505-84-7 |
| Formula | C17H14ClF2N3O3S |
| M. Wt | 413.8 |
| Purity | >98% |
| Synonyms | PLX4720 |
| SMILES | CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=NC=C(C=C23)Cl)F |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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