PF-05212384, also known as PKI-587 and Gedatolisib, is a dual phosphatidylinositol-3-kinase (PI3K) / mammalian target of rapamycin (mTOR) inhibitor. PKI-587 potently inhibited class I PI3Ks (IC50 vs PI3K-A = 0.4 nM), PI3K-A mutants, and mTOR. PF-05212384 inhibited growth of 50 diverse human tumor cell lines at IC50s ﹤100 nM and has been in clinical trials in patients with advanced solid tumors. PF-05212384 has also been found to sensitize cells to radiation.
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