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PP-121

Catalog No.S2622 1 Review(s)
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PP-121 Chemical Structure

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Biological Activity

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]

References on PP-121
  • [1] Nat Chem Biol. 2008;4(11): 691–699
Molecular Weight (WM): 319.36
Formula:

C17H17N7

CAS No.: 1092788-83-4
Synonyms:
N/A
Dissolve in (25°C): DMSO ≥64mg/mL 
Water <1mg/mL 
Ethanol ≥2mg/mL 
Storage: 2 years-20°CPowder
1 week-4°Cin DMSO
1 month-80°in DMSO

Quality Control & MSDS

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COA H-NMR HPLC
Notes:

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    After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of PP-121 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

  • After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of PP-121 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

  • Data independently produced by Dr. Zhang of Tianjin Medical University
    PP-121 purchased from Selleck

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After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of PP-121 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

Data independently produced by Dr. Zhang of Tianjin Medical University

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