Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Everolimus is a derivative of Rapamycin (sirolimus), it is a mTOR inhibitor that binds with high affinity to the FK506 binding protein-12 (FKBP-12), thereby forming a drug complex that inhibits the activation of mTOR. This inhibition reduces the acti...
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Temsirolimus is an intravenous drug for the treatment of renal cell carcinoma (RCC), developed by Wyeth Pharmaceuticals and approved by the FDA in late May 2007, and was also approved by the European Medicines Agency (EMEA) on November 2007. It is a ...
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR, originally being developed by Wyeth. Upon intravenous administration, gedatolisib inhibits both PI3K and mTOR kinases, which may result in apoptosis and gr...
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Sonolisib (PX-866) is a small-molecule inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity. Sonolisib inhibits the production of the secondary messenger phosphatidylinositol-3,4...
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
VS-5584 is a potent and selective oral small molecule inhibitor of all 4 PI3K isoforms and mTORC1 and mTORC2. VS-5584 inhibits mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively. Verastem has patent protection of VS-5584 through 2029, ...
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
CC-223 is an orally available inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor CC-223 inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a de...
Class (Stereo):
CHEMICAL (ACHIRAL)
PQR-309 is an orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity. PI3K/mTOR kinase inhibitor PQR-309 inhibits the PI3K kinase isofor...
Class (Stereo):
CHEMICAL (ACHIRAL)
CC-115 is a recently identified inhibitor of the mammalian Target of Rapamycin Kinase (TORK) and DNA-Dependent Protein Kinase (DNA-PK). It is under investigation in phase II clinical trials for the treatment for Glioblastoma and in phase I trials fo...
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
GSK 1059615, a pyridinylquinoline derivative, is a novel PI3K kinase and mTOR dual inhibitor. GSK1059615 was in phase I clinical trial in patients with solid tumors or lymphoma, but this study was terminated prematurely due to lack of sufficient expo...
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
PKI-179 is an orally efficacious dual PI3K/mTOR inhibitor, possessing antineoplastic activity. The key residues involved in binding of PKI-179 were Ala-805 in PI3Kγ and Ile-2163 in mTOR as they have lost maximum accessible surface area due to binding...