PP-121 Chemical Structure
Linifanib (ABT869) is a structurally novel, potent RTK and VEGF and PDGF receptor families inhibitor for, PDGFR-β, KDR, and CSF-1R, with IC50 of 0.2 nM, 2 nM, 4 nM, and 7 nM, respectively.
Axitinib (AG-013736) is a multiple receptor kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-β and c-KIT with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.
BEZ235 (NVP-BEZ235)is a dual ATP-competitive phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM,respectively.
BIBF1120 (Vargatef) is a potent VEGF receptor (VEGFR), PDGFR and FGFR kinase inhibitor for VEGFR1, VEGFR2, VEGFR3 with IC50 of 34 nM, 5 nM and 5 nM, respectively.
Deforolimus (Ridaforolimus) is a small-molecule inhibitor of mTOR.
Imatinib Mesylate is a multitargeted c-kit, PDGF-R and c-ABL inhibitor with IC50 of 3.9 and 2.9 μM for the inhibition of T-cell proliferation stimulated by DCs and PHA, respectively.
Motesanib (AMG-706) is a multiple inhibitor of VEGFR1/2/3(IC50: 2 ηM /3 ηM /6 ηM),PDGFR (84ηM), kit (8ηM), and Ret (59ηM)receptors
Pazopanib HCl is a VEGFR inhibitor, IC50 of 10, 30 and 47 nM for VEGFR-1, -2, and -3.
PI-103 is a potent, cell-permeable, ATP-competitive PI3K family member inhibitor with IC50 of 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β, and p110γ, respectively.
Rapamycin also known as Sirolimus & Rapamune is an mTOR inhibitor. Rapamycin Sirolimus inhibits cell motility by suppression of mTOR-mediated pathways.
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]
| Molecular Weight (WM): | 319.36 |
|---|---|
| Formula: | C17H17N7 |
| CAS No.: | 1092788-83-4 |
| Synonyms: |
N/A
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| 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 |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
A collection of 426 FDA approved drugs
A collection of 139 natural products
A collection of 40 chemotherapeutic agents
A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules

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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