Gedatolisib

Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively[1]. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2[2].

Product Specifications

CAS Number

[1197160-78-3]

Product Name Alternative

PKI-587; PF-05212384

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

MTOR; PI3K

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PKI-587.html

Purity

99.84

Solubility

DMSO : 4 mg/mL (warming) |H2O : < 0.1 mg/mL

Smiles

CN(C1CCN(C(C2=CC=C(NC(NC3=CC=C(C4=NC(N5CCOCC5)=NC(N6CCOCC6)=N4)C=C3)=O)C=C2)=O)CC1)C

Molecular Formula

C32H41N9O4

Molecular Weight

615.73

Precautions

H302, H315, H319, H335

References & Citations

[1]Venkatesan AM, et al. Bis (morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. J Med Chem. 2010, 53 (6), 2636-2645.|[2]Freitag H, et al. Inhibition of mTOR's Catalytic Site by PKI-587 Is a Promising Therapeutic Option for Gastroenteropancreatic Neuroendocrine Tumor Disease. Neuroendocrinology. 2017;105 (1) :90-104.