PKI-179

• Description:

  PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo[1][2].

• UNSPSC:

  12352005

• 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-179.html

• Purity:

  98.0

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  O=C (NC1=CC=NC=C1) NC2=CC=C (C3=NC (N4C5CCC4COC5) =NC (N6CCOCC6) =N3) C=C2

• Molecular Formula:

  C25H28N8O3

• Molecular Weight:

  488.54

• References & Citations:

  [1]Venkatesan AM, et, al. PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K) /mammalian target of rapamycin (mTOR) inhibitor. Bioorg Med Chem Lett. 2010 Oct 1;20 (19) :5869-73.|[2]Rehan M. A structural insight into the inhibitory mechanism of an orally active PI3K/mTOR dual inhibitor, PKI-179 using computational approaches. J Mol Graph Model. 2015 Nov;62:226-234.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 1

• Isoform:

  MTOR; PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ

• CAS Number:

  1197160-28-3