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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
MTOR; mTORC1; mTORC2; PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ
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