生物活性
PLX4032(Vemurafenib)也称为RG7204，Vemurafenib，R7204，RO5185426。PLX4032是B-raf抑制剂，IC50为44 nM。
Targets
| Target | Value |
| SRMS | IC50: 18nM |
| ACK1 | IC50: 19nM |
| B-Raf(V600E) | IC50: 31nM |
| C-Raf | IC50: 48nM |
| MAP4K5(KHS1) | IC50: 51nM |
| FGR | IC50: 63nM |
| B-Raf | IC50: 100nM |
| LCK | IC50: 183nM |
| BRK | IC50: 213nM |
| NEK11 | IC50: 317nM |
| BLK | IC50: 547nM |
| LynB | IC50: 599nM |
| YES1 | IC50: 604nM |
| WNK3 | IC50: 877nM |
| MNK2 | IC50: 1.717μM |
| FRK(PTK5) | IC50: 1.884μM |
| CSK | IC50: 2.339μM |
| Src | IC50: 2.389μM |
化学数据
| 目录号 | A10739 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 489.9 |
| Formula | C23H18ClF2N3O3S |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 918504-65-1 |
| Synonyms | RG7204,RO5185426,Zelboraf, PLX-4032 |
| SMILES | CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=NC=C(C=C23)C4=CC=C(C=C4)Cl)F |
溶解度
| In vitro (25°C) | DMSO | 83 mg/mL (169.41 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 4% DMSO+30% PEG 300+5% Tween 80+ddH2O (suspension) | 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 20.41 mL | 102.06 mL | 204.12 mL |
| 0.5 mM | 4.08 mL | 20.41 mL | 40.82 mL |
| 1 mM | 2.04 mL | 10.21 mL | 20.41 mL |
| 5 mM | 0.41 mL | 2.04 mL | 4.08 mL |
*The above data is based on the productmolecular weight 489.9 . 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.
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