GSK2126458
| CAS No. | 1086062-66-9 | Cat. No. | BCP02252 |
| Name | GSK2126458 | ||
| Synonyms | GSK-2126458;GSK 2126458; Omipalisib; | ||
| Formula | C25H17F2N5O3S | M. Wt | 505.5 |
| Description | GSK2126458 potently inhibits the activity of common activating mutants of p110α (E542K, E545K, and H1047R) found in human cancer with Ki of 8 pM, 8 pM and 9 pM, respectively.GSK2126458 causes a significant reduction in the levels of pAkt-S473 with remarkable potency in T47D and BT474 cells with IC50 of 0.41 nM and 0.18 nM, respectively. Furthermore, GSK2126458 leads to a G1 cell cycle arrest and produces the inhibitory effect on cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines with IC50 of 3 nM and 2.4 nM, respectively. | ||
| Pathways | PI3K/Akt/mTOR | ||
| Targets | PI3K mTOR | ||
Structure
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