AZD-8835

Description	IC50 value: 5.7 nM (PI3Kδ), 6.2 nM (PI3Kα) Target: PI3K in vitro: AZD8835 is a orally bioavailable inhibitor of the class I (PI3K) catalytic subunit alpha (PIK3CA), with potential antineoplastic activity. PI3K alpha inhibitor AZD8835 selectively binds to and inhibits PIK3CA and its mutated forms, in the PI3K/Akt (protein kinase B)/mammalian target of rapamycin (mTOR) pathway. This results in both apoptosis and growth inhibition in PIK3CA-expressing tumor cells. By specifically targeting PIK3CA, this agent may be more efficacious and less toxic than pan-PI3K inhibitors. Dysregulation of the PI3K/Akt/mTOR pathway is often found in solid tumors and results in the promotion of tumor cell growth, survival, and resistance to chemo- and radio-therapy. PIK3CA, one of the most frequently mutated oncogenes, encodes the p110-alpha catalytic subunit of the class I PI3K. In vivo: AZD8835 shows pharmacodynamic modulation of AKT phosphorylation and near complete inhibition of tumour growth (93% tumou
Pathways	PI3K/Akt/mTOR
Targets	PI3K

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