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PLX-4720是一种有效的，选择性的B-RafV600E抑制剂，无细胞试验中IC50为13 nM，同样有效地作用于c-Raf-1(Y340D和Y341D突变型)，作用于B-RafV600E比作用于野生型B-Raf选择性高10倍。
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.
| 目录号 | A10002 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 413.8 |
| Formula | C17H14ClF2N3O3S |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 918505-84-7 |
| Synonyms | PLX4720 |
| SMILES | CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=NC=C(C=C23)Cl)F |
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