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PF-04217903 methanesulfonate is a potent ATP-competitive inhibitor of c-Met kinase (Ki of 4.8 nM for human c-Met).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $49 | 5 days | |
5 mg | $77 | 7-10 days |
Description | PF-04217903 methanesulfonate is a potent ATP-competitive inhibitor of c-Met kinase (Ki of 4.8 nM for human c-Met). |
Targets&IC50 | c-Met (human):ki:4.8 nM |
In vitro | PF-04217903 induces apoptosis of GTL-16 cells (IC50=31 nM) [1]. PF-04217903 methanesulfonate also inhibits HGF-mediated cell migration and Matrigel invasion in several c-Met–overexpressing tumor cell lines such as human NCI-H441 lung carcinoma and HT29 colon carcinoma with IC50 values comparable with those for inhibition of c-Met phosphorylation in these cell lines (IC50= 7-12.5 nM)[1]. |
In vivo | PF-04217903 methanesulfonate 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 methanesulfonate strongly induces phospho-PDGFRβ levels in U87MG xenograft tumors[1]. |
Molecular Weight | 468.49 |
Formula | C20H20N8O4S |
Cas No. | 956906-93-7 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (106.73 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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