General description

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.

Legal Information

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

Other Notes

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.

Packaging

2 mg in Plastic ampoule

Packaged under inert gas

Physical form

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

Reconstitution

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

Warning

Toxicity: Irritant (B)