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PF-04217903 phenolsulfonate is a potent, ATP-competitive inhibitor of c-Met kinase with a Ki of 4.8 nM for human c-Met.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | Backorder |
Description | PF-04217903 phenolsulfonate is a potent, ATP-competitive inhibitor of c-Met kinase with a Ki of 4.8 nM for human c-Met. |
Targets&IC50 | c-Met (human):ki:4.8 nM |
In vitro | PF-04217903 phenolsulfonate inhibits proliferation of c-Met–amplified human GTL-16 gastric carcinoma and H1993 NSCLC cells with IC50 values of 12 and 30 nM, respectively[1]. |
In vivo | PF-04217903 phenolsulfonate shows a significant dose-dependent reduction of human IL-8 levels in both the U87MG and GTL-16 models and decreases human VEGFA levels in the GTL-16 model. PF-04217903 phenolsulfonate strongly induces phospho-PDGFRβ levels in U87MG xenograft tumors.PF-04217903 phenolsulfonate dose dependently inhibits c-Met, Gab-1, Erk1/2, and AKT phosphorylation and induced apoptosis (cleaved caspase-3) in U87MG xenograft tumors at all dose levels.[1]. |
Molecular Weight | 546.56 |
Formula | C25H22N8O5S |
Cas No. | 1159490-85-3 |
Relative Density. | 1.31g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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