SAR245409 (CAS: 934493-76-2) is a potent and highly selective pan inhibitor of class I PI3Ks (α/β/γ/δ, IC50=39/110/9/43 nM) with activity against mTOR(IC50=160-910 nM). Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated in a PI3K-independent fashion in response to nutrient and energy deprivation. Accordingly, this agent maybe more potent compared to an agent that inhibits either PI3K kinase or mTOR kinase alone.
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