生物活性
GSK2126458 (Omipalisib)是一种高选择性的，有效的p110α/β/γ/δ和 mTORC1/2抑制剂，无细胞试验中Ki分别为0.019 nM/0.13 nM/0.024 nM/0.06 nM和0.18 nM/0.3 nM。
Targets
| Target | Value |
| p110α | ki: 0.019nM |
| p110δ | ki: 0.024nM |
| p110γ | ki: 0.06nM |
| p110β | ki: 0.13nM |
| mTORC1 | ki: 0.18nM |
| mTORC2 | ki: 0.3nM |
化学数据
| 目录号 | A11035 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 505.5 |
| Formula | C25H17F2N5O3S |
| 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. | 1086062-66-9 |
| Synonyms | GSK-2126458 |
| SMILES | COC1=C(C=C(C=N1)C2=CC3=C(C=CN=C3C=C2)C4=CN=NC=C4)NS(=O)(=O)C5=C(C=C(C=C5)F)F |
溶解度
| In vitro (25°C) | DMSO | 96 mg/mL (189.91 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 2% DMSO+40% PEG 300+2% Tween 80+ddH2O | 3 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 | 19.78 mL | 98.91 mL | 197.82 mL |
| 0.5 mM | 3.96 mL | 19.78 mL | 39.56 mL |
| 1 mM | 1.98 mL | 9.89 mL | 19.78 mL |
| 5 mM | 0.4 mL | 1.98 mL | 3.96 mL |
*The above data is based on the productmolecular weight 505.5 . 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.
