Chemical Name: 2,4-Difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]benzenesulfonamide
Biological ActivityHighly potent PI 3-K inhibitor (IC50 = 0.04 nM). Also inhibits mTOR (Ki = 0.18 - 0.3 nM) and DNA-PK (IC50 = 0.28 nM). Induces G1 cell cycle arrest and inhibits proliferation of some breast cancer cells lines in vitro. Reduces pAKT-S473 levels in and inhibits growth of BT474 breast cancer xenografts in mice. Orally bioavailable.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of GSK2126458, a highly potent inhibitor of PI3K and the mammalian target of rapamycin.
Knight et al.
ACS Med.Chem.Lett., 2010;1:39
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