BEZ 235

BEZ235 is a dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. BEZ235 inhibits both mTORC1 and mTORC2.

Dactolisib is an imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor, a mTOR inhibitor and an antineoplastic agent. It is an imidazoquinoline, a nitrile, a member of quinolines, a ring assembly and a member of ureas.|Dactolisib has been used in trials studying the treatment of Cancer, Solid Tumor, Renal Cancer, Breast Cancer, and Cowden Syndrome, among others.|Dactolisib is an orally bioavailable imidazoquinoline targeting the phosphatidylinositol 3 kinase (PI3K) and the mammalian target of rapamycin (mTOR), with potential antineoplastic activity. Dactolisib inhibits PI3K kinase and mTOR kinase in the PI3K/AKT/mTOR kinase signaling pathway, which may result in tumor cell apoptosis and growth inhibition in PI3K/mTOR-overexpressing tumor cells. 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 independent of PI3K.

Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. NVP-BEZ235 is a potent dual inhibitor of PI3K and mTOR that is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents when used in in vivo combination studies. It inhibits PI3K isoforms and mutants with low nanomolar IC50 values, leading to growth arrest in the G1 phase. Through its effects on PI3K, NVP-BEZ235 inhibits VEGF-induced angiogenesis. By directly blocking cell growth and indirectly inhibiting angiogenesis, it has potential in both solid tumors and in metastatic melanoma therapy.[Cayman Chemical]

Molecular Weight:469.5
XLogP3:5.2
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:3
Exact Mass:469.19026037
Monoisotopic Mass:469.19026037
Topological Polar Surface Area:73.1
Heavy Atom Count:36
Complexity:872
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes