A cell-permeable pyrazolopyrimidine compound that effectively targets the ATP pocket of both protein tyrosine kinases (IC₅₀<0.26 M against Abl, EGFR, EphB4, Hck, PDGFR, RET, Src, Src^T338I, and VEGFR2) and PI 3-K family kinases (IC₅₀<1.4 M against p110α/ β/ δ/ γ, mTOR, and DNA-PK). PP121 is less effective against ser/thr kinases and exhibits significant inhibition of only 14 ser/thr kinases (≥70% inhibition with 1 M inhibitor and 10 M ATP) in a 219 kinase panel screening. Individually targeting Ret by sorafenib (IC₅₀ = 780 nM) or PI 3-K/mTOR pathway by PI-103 (IC₅₀ = 800 nM) is shown to be less effective than PP121 treatment (IC₅₀ = 50 nM) in inhibiting the proliferation of Ret C634W-expressing TT thyroid carcinoma cultures.

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Apsel, B., et al. 2008. Nat. Chem. Biol.4, 691.

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