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PP121 is a dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR). PP121 is the first inhibitor active on both Tyrosine kinases and the phosphatidylinositol-3-OH kinase (PI(3)K) family. PP121 blocks the proliferation of tumor cells by direct inhibition of PI 3-K, mTOR, Src and the VEGF receptor. PP-121 induces a G0/G1 arrest in LN220, U87 and Seg1 cells. PP-121 directly inhibits Bcr-Abl induced tyrosine phosphorylation, resulting in drug-induced apoptosis in K562 cells and a combination of apoptosis and cell cycle arrest in Bcr-Abl expressing BaF3 cells. PP-121 also inhibits other PI3Ks including p110α and DNA-PK with IC50 of 52 nM and 60 nM, respectively.
| Cell Experiment | |
|---|---|
| Cell lines | U87 and LN229 cells line |
| Preparation method | Cell proliferation assays. Cells grown in 96-well plates were treated with inhibitor at 4-fold dilutions (10 µM - 0.040 μM) or vehicle (0.1% DMSO). After 72 h cells were exposed to Resazurin sodium salt (22 µM, Sigma) and fluorescence was quantified. IC50 values were calculated using Prism software. For proliferation assays involving single cell counting, non-adherent cells were plated at low density (3–5% confluence) and treated with drug (2.5 µM) or vehicle (0.1% DMSO). Cells were diluted into trypan blue daily and viable cells counted using a hemocytometer. |
| Concentrations | 10 µM - 0.040 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Eca-109 cells Mice xenograft |
| Formulation | 10% 1-methyl-2-pyrrolidinone and 90% PEG 300 |
| Dosages | 30 mg/kg daily for 30 days |
| Administration | oral gavage |
| Molecular Weight | 319.36 |
| Formula | C17H17N7 |
| CAS Number | 1092788-83-4 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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