PKI-179
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].
Product Specifications
CAS Number
1197160-28-3
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
Available Sizes
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