PKI-179 (hydrochloride)

PKI-179 hydrochloride 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 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo[1][2].

Product Specifications

CAS Number

[1463510-35-1]

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-hydrochloride.html

Concentration

10mM

Purity

99.66

Solubility

DMSO : 20 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C25H29ClN8O3

Molecular Weight

525.00

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.