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 -20?C, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20?C 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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