生物活性
GSK1120212 (JTP-74057,Trametinib)强烈阻止了MEK1和MEK2激酶的活性，而不是其他98种激酶的活性。
靶点信息
| MEK1 (Cell-free assay) | MEK2 (Cell-free assay) | | | |
| 0.92 nM | 1.8 nM | | | |
化学数据
| 目录号 | A11029 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 615.4 |
| Formula | C26H23FIN5O4 |
| 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. | 871700-17-3 |
| Synonyms | GSK-1120212, GSK212, Trametinib |
| SMILES | CC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC(=CC=C4)NC(=O)C)C5CC5 |
溶解度
| In vitro (25°C) | DMSO | Warmed: 19 mg/mL (30.87 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 4% DMSO+corn oil | 2 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 | 16.25 mL | 81.25 mL | 162.5 mL |
| 0.5 mM | 3.25 mL | 16.25 mL | 32.5 mL |
| 1 mM | 1.62 mL | 8.12 mL | 16.25 mL |
| 5 mM | 0.32 mL | 1.62 mL | 3.25 mL |
*The above data is based on the productmolecular weight 615.4 . 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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