生物活性
GDC-0973 (Cobimetinib,RG7420)是一种有效且高度选择性的MEK1抑制剂，IC50为4.2 nM，对MEK1的选择性选择性是对MEK2的100倍以上，并且当针对一组超过100个丝氨酸的抑制剂进行测试时，没有显示出明显的抑制作用。
靶点信息
化学数据
| 目录号 | A11441 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 530.1 |
| Formula | C21H21F3IN3O2 |
| 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. | 934660-93-2 |
| Synonyms | XL518, XL 518, XL-518, RG7420 |
| SMILES | C1CCN[C@@H](C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O |
溶解度
| In vitro (25°C) | DMSO | 88 mg/mL (165.62 mM) |
| Water | Insoluble |
| Ethanol | Warmed: 41 mg/mL (77.17 mM) |
| In vivo | 5% DMSO+30% 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 18.86 mL | 94.32 mL | 188.64 mL |
| 0.5 mM | 3.77 mL | 18.86 mL | 37.73 mL |
| 1 mM | 1.89 mL | 9.43 mL | 18.86 mL |
| 5 mM | 0.38 mL | 1.89 mL | 3.77 mL |
*The above data is based on the productmolecular weight 530.1 . 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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