产品
编 号：F050488
分子式：C25H22N8O5S
分子量：546.56
分子式：C25H22N8O5S
分子量：546.56
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CAS No: 1159490-85-3
产品详情
生物活性：
PF-04217903 phenolsulfonate is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 phenolsulfonate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties.
体内研究：
PF-04217903 phenolsulfonate (1-30 mg/kg; p.o.; daily for 16 days) shows dose-dependent tumor growth inhibition, which correlated with the inhibition in c-Met phosphorylation in these tumors.PF-04217903 phenolsulfonate (5-50 mg/kg, p.o.; once daily for 3 days) 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. 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.Animal Model:Female nu/nu mice (GTL-16 xenograft model)
Dosage:1, 3, 10, 30 mg/kg
Administration:Oral; daily for 16 days
Result:Showed dose-dependent tumor growth inhibition, and was correlated with the inhibition in c-Met phosphorylation in these tumors.
体外研究：
PF-04217903 phenolsulfonate (0.1-10000 nM; 48-72 hours) inhibits proliferation of c-Met–amplified human GTL-16 gastric carcinoma and H1993 NSCLC cells with IC50 values of 12 and 30 nM, respectively.PF-04217903 phenolsulfonate (1.5-3333 nM; 48 hours) induces apoptosis of GTL-16 cells (IC50=31 nM).PF-04217903 phenolsulfonate 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).PF-04217903 phenolsulfonate displays similar potency to inhibit the activity of c-Met-H1094R, c-Met-R988C, and c-Met-T1010I with IC50 of 3.1 nM, 6.4 nM, and 6.7 nM, respectively. PF-04217903 phenolsulfonate has no inhibitory activity against c-Met-Y1230C with IC50 of >10 μM.
PF-04217903 phenolsulfonate is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 phenolsulfonate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties.
体内研究：
PF-04217903 phenolsulfonate (1-30 mg/kg; p.o.; daily for 16 days) shows dose-dependent tumor growth inhibition, which correlated with the inhibition in c-Met phosphorylation in these tumors.PF-04217903 phenolsulfonate (5-50 mg/kg, p.o.; once daily for 3 days) 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. 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.Animal Model:Female nu/nu mice (GTL-16 xenograft model)
Dosage:1, 3, 10, 30 mg/kg
Administration:Oral; daily for 16 days
Result:Showed dose-dependent tumor growth inhibition, and was correlated with the inhibition in c-Met phosphorylation in these tumors.
体外研究：
PF-04217903 phenolsulfonate (0.1-10000 nM; 48-72 hours) inhibits proliferation of c-Met–amplified human GTL-16 gastric carcinoma and H1993 NSCLC cells with IC50 values of 12 and 30 nM, respectively.PF-04217903 phenolsulfonate (1.5-3333 nM; 48 hours) induces apoptosis of GTL-16 cells (IC50=31 nM).PF-04217903 phenolsulfonate 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).PF-04217903 phenolsulfonate displays similar potency to inhibit the activity of c-Met-H1094R, c-Met-R988C, and c-Met-T1010I with IC50 of 3.1 nM, 6.4 nM, and 6.7 nM, respectively. PF-04217903 phenolsulfonate has no inhibitory activity against c-Met-Y1230C with IC50 of >10 μM.
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