Gedatolisib

• Description :

  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 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

• CAS Number :

  [1197160-78-3]