1025065-69-3

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

PP121 is a multitargeted dual receptor tyrosine kinases inhibitor with IC50 of 0.052, 1.4, 0.15, 1.1, 0.06, 0.01and 0.002 μM for p110α, p110β, p110δ, p110γ, DNA-PK, mTOR and PDGFR, respectively. PP121 also inhibits Abl, Hck, Src,Src(T338I), VEGFR2, EGFR EphB4 with IC50 of 0.018, 0.008, 0.014, 0.22, 0.012, 0.26, 0.19 μM, respectively. PP121 exhibits no significant effect on receptor serine/threonine kinases (RSTKs). PP121 blocks the proliferation of tumor cells by direct inhibition of PI 3-K, mTOR, Src and the VEGF receptor. PP121 achieves its dual potency by targeting a residue (Glu310 in Src) that has been structurally conserved between kinase families. PP121 potently and dose-dependently blocked the phosphorylation of Akt, p70S6K and S6 in these cells. ^[1]

参考文献

[1] Apsel B et al. Nat Chem Biol. 2008 Nov;4(11):691-9.