生物活性
Dabrafenib (GSK2118436A)是一种有效且选择性的B-RAF蛋白激酶抑制剂，具有V600E突变，目前正在临床试验中。
靶点信息
| B-Raf (V600E) (Cell-free assay) | B-Raf (Cell-free assay) | C-Raf (Cell-free assay) | | |
| 0.8 nM | 3.2 nM | 5.0 nM | | |
化学数据
| 目录号 | A11381 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 519.6 |
| Formula | C23H20F3N5O2S2 |
| 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. | 1195765-45-7 |
| Synonyms | GSK2118436A |
| SMILES | CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F |
溶解度
| In vitro (25°C) | DMSO | 28 mg/mL (53.89 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 2% DMSO+45% PEG 300+2% 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 | 19.25 mL | 96.23 mL | 192.46 mL |
| 0.5 mM | 3.85 mL | 19.25 mL | 38.49 mL |
| 1 mM | 1.92 mL | 9.62 mL | 19.25 mL |
| 5 mM | 0.38 mL | 1.92 mL | 3.85 mL |
*The above data is based on the productmolecular weight 519.6 . 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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