A cell-permeable pyrazolopyrimidine compound that effectively targets the ATP pocket of both protein tyrosine kinases (IC50<0.26uM against Abl, EGFR, EphB4, Hck, PDGFR, RET, Src, SrcT338I, and VEGFR2) and PI 3-K family kinases (IC50<1.4uM against p110a/ b/ d/ g, 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 1uM inhibitor and 10uM ATP) in a 219 kinase panel screening. Individually targeting Ret by sorafenib (IC50=780nM) or PI 3-K/mTOR pathway by PI-103 (IC50=800nM is shown to be less effective than PP121 treatment (IC50=50nM) in inhibiting the proliferation of Ret C634W-expressing TT thyroid carcinoma cultures.
Synonyms:1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, PI 3-K/mTOR Inhibitor II, VEGFR Tyrosine Kinase Inhibitor XXXII, VEGFR2 Kinase Inhibitor XXX, mTOR Inhibitor VII, PI 3-K Inhibitor XIII, Abl Inhibitor IV, PDGFR Tyrosine Kinase Inhibitor XVIII
Formula:C17H17N7
Molecular Weight:319.4
Solubility:DMSO
Storage and Stability:Store at 4°C. Caution: Light-sensitive. For maximum recovery of product, centrifuge the original vial prior to removing the cap.