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Biological Activity
GSK2126458 is a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.
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 |
| 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. |
|||
| 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.
| Catalog Num | A11035 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 1086062-66-9 |
| Formula | C25H17F2N5O3S |
| M. Wt | 505.5 |
| Purity | >98% |
| 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 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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