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Signal Inhibitors and Activators
PP-121
$292.8/ 10mg
QuantityTotal: $293
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Product Information
Kinase Inhibitor Name PP-121
FormulaC17H17N7
SolubilityDMSO ≥64 mg/mL Water <1 mg/mL Ethanol ≥2 mg/mL
Stability:
2 years -20℃ Powder
1 week -4℃ in DMSO
1 month -80℃ in DMSO
Stability:
2 years -20℃ Powder
1 week -4℃ in DMSO
1 month -80℃ in DMSO
CAS No.1092788-83-4
Biological ActivityPP121 is a multitargeted dual receptor tyrosine kinases inhibitor with IC50 of 0.052, 1.4, 0.15, 1.1, 0.06, 0.01and 0.002 μM for p110α, p110β, p110δ, p110γ, DNA-PK, mTOR and PDGFR, respectively. PP121 also inhibits Abl, Hck, Src,Src(T338I), VEGFR2, EGFR EphB4 with IC50 of 0.018, 0.008, 0.014, 0.22, 0.012, 0.26, 0.19 μM, respectively. PP121 exhibits no significant effect on receptor serine/threonine kinases (RSTKs). PP121 blocks the proliferation of tumor cells by direct inhibition of PI 3-K, mTOR, Src and the VEGF receptor. PP121 achieves its dual potency by targeting a residue (Glu310 in Src) that has been structurally conserved between kinase families. PP121 potently and dose-dependently blocked the phosphorylation of Akt, p70S6K and S6 in these cells. [1]
M.W.319.36
ReferencesTargeted polypharmacology: Discovery of dual inhibitors of tyrosine and phosphoinositide kinases Beth Apsel,Jimmy A. Blair,et al. Nat Chem Biol. 2008;4(11): 691–699
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.
Price292.8$
Research AreaStem Cells Cancer Cardiovascular Cell Biology Epigenetics & Nuclear Signaling Developmental Biologys Immunology Drug Discovery Products Metabolism Neuroscience Signal Transduction
multitargeted dual receptor tyrosine kinases inhibitor with IC50 of 0.052, μM for p110α, p110β, p110δ, p110γ, DNA-PK, mTOR and PDGFR, Abl, Hck, Src,Src(T338I), VEGFR2, EGFR EphB4 with IC50 of 0.018, 0.19 μM, respectively. PP121 exhibits no significant effect on receptor PP121 blocks the proliferation of tumor cells by direct inhibition of PI 3-K, receptor. PP121 achieves its dual potency by targeting a residue (Glu310 in
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