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GSK 2126458
- Omipalisib
- Soluble in DMSO
- MF: C25H17F2N5O3S
- MW: 505.5
Description
GSK 2126458 (Omipalisib) is a highly potent, orally bioavailable dual PI3K/mTOR inhibitor with subnanomolar reported Ki values across class I PI3K isoforms.
PI3K and mTOR signaling integrate growth-factor input with metabolism, survival and protein synthesis. GSK 2126458 is useful for studying pathway blockade in PI3K-dependent cancer models and for comparing catalytic PI3K/mTOR inhibition with more selective pathway inhibitors.
Key Features
- Dual inhibitor of PI3K and mTOR
- Subnanomolar reported potency against class I PI3K isoforms
- Suppresses PI3K/AKT/mTOR growth signaling
- Orally bioavailable compound for oncology model research
Applications
- PI3K/mTOR pathway studies
- Cancer cell proliferation and survival assays
- Kinase inhibitor profiling
- Drug combination and resistance research
More Information
| Parent CAS No. | 1086062-66-9 |
|---|---|
| Chemical Name | 2,4-difluoro-N-(2-methoxy-5-(4-(pyridazin-4-yl)quinolin-6-yl)pyridin-3-yl)benzenesulfonamide |
| SMILES | C1C=C(S(=O)(=O)NC2C(OC)=NC=C(C3C=C4C(C5C=CN=NC=5)=CC=NC4=CC=3)C=2)C(F)=CC=1F |
| MFCD | MFCD16038929 |
| InChi | InChI=1S/C25H17F2N5O3S/c1-35-25-23(32-36(33,34)24-5-3-18(26)12-21(24)27)11-17(13-29-25)15-2-4-22-20(10-15)19(7-8-28-22)16-6-9-30-31-14-16/h2-14,32H,1H3 |
| InChiKey | CGBJSGAELGCMKE-UHFFFAOYSA-N |
| CID | 25167777 |
| Short Description | PI3K/mTOR inhibitor |
References
- SD Knight et al. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med. Chem. Lett. 2010, 1(1), 39–43.
- E Leung et al. Comparison of the effects of the PI3K/mTOR inhibitors NVP-BEZ235 and GSK2126458 on tamoxifen-resistant breast cancer cells. Cancer Biol. Ther. 2011, 11(11), 938-946.
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