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Characteristics
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Cell-permeable. A highly potent, pan phosphoinositide 3-kinase (PI 3-K) family kinase inhibitor with biochemical Ki,'s of 0.019 nM (PI 3-Kbeta), 0.13 nM (PI 3-Kbeta), 0.024 nM (PI 3-Kdelta), 0.06 nM (PI 3-Kalpha), 0.18 nM (mTORC1), and 0.3 nM (mTORC2). In vivo, GSK2126458 displays anti-tumor activity in both pharmacodynamic and tumor growth efficacy models.
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