PI-103

Toxicity: Irritant (B)

A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR (IC₅₀ = 2, 8, 88, 48, 150, 26, 20, and 83 nM for DNA-PK, p110α, p110β, p110δ, p110γ, PI3-KC2β, mTORC1, and mTORC2, respectively). It inhibits ATR and ATM only at much higher concentrations (IC₅₀ = 850 and 920 nM, respectively) and exhibits little activity towards a panel of more than 40 other kinases even at concentrations as high as 10 µM. Shown to effectively block PI3-K/Akt signaling and cell proliferation in glioma cell lines both in vitro and in vivo.

Raynaud, F.I., et al. 2007. Cancer Res.67, 5840.
Fan, Q.W., et al. 2006. Cancer Cell9, 341.
Knight, Z.A., et al. 2006. Cell125, 733.

Packaged under inert gas

A 10 mM (2 mg/574 µl) solution of PI-103 (Cat. No. 528100) in DMSO.

Following initial thaw, aliquot and freeze (-20°C).

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany