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pp121 Tyrosin Kinase and PI3K Pathway Inhibitor

Catalog # CD0257

Price:  1 mg - $35; 5 mg - $55; 10 mg - $75; 25 mg - $130; 50 mg - $220; 100 mg - $395; 200 mg - $750

Availability:  In stock





White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. Purity: 99% by HPLC. CAS# 1092788-83-4. Solubility: DMSO (100 mg/mL), ethanol (50 mg/mL). Molecular Formula: C17H17N7. Molecular Weight: 319.4.



A cell-permeable pyrazolopyrimidine compound that effectively targets the ATP pocket of both protein tyrosine kinases (IC50 <0.26 μM against Abl, EGFR, EphB4, Hck, PDGFR, RET, Src, Src, and VEGFR2) and PI3-K T338I family kinases (IC50 <1.4 μM 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 μM inhibitor and 10 mM ATP) in a 219 kinase panel screening. Individually targeting Ret by sorafenib (IC50 = 780 nM) or PI3-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. 


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





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Caution Not fully tested. For research use only. Not for human use.

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