PKI-402

PKI-402 is a potent, selective, ATP-competitive, small molecule inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms (alpha, beta, gamma, delta) and mammalian target of rapamycin (mTOR)[1][3][5][6]. It inhibits PI3Kα/β/γ/δ with nanomolar potency (IC50: 2 nM, 7 nM, 16 nM, 14 nM, respectively) and mTOR (IC50: 3 nM)[1]. PKI-402 is typically used as a biochemical tool in preclinical research to study PI3K/mTOR signaling, a pathway highly relevant to cancer cell proliferation, survival, metastasis, and resistance to therapies[1][5][7]. In preclinical models, PKI-402 shows anti-tumor activity in a variety of cancers, including breast and ovarian, by inducing apoptosis and inhibiting tumor growth[1][2][7]. It can sensitize cells to irradiation and block breast cancer-induced osteolysis by disrupting PI3K/AKT/mTOR signal transduction[2][6]. There are no known brand or trade names.

Other names

1-[4-(3-ethyl-7-morpholin-4-yltriazolo[4,5-d]pyrimidin-5-yl)phenyl]-3-[4-(4-methylpiperazine-1-carbonyl)phenyl]urea