| 品牌 | 货号 | 产品规格 | 价格(RMB) | 库存（上海） | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
| 源叶(MedMol) | S87543-5mg | 98% | ￥210.00元 | 预计交期：2-3天 | - | - | - |
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| 源叶(MedMol) | S87543-10mg | 98% | ￥380.00元 | 预计交期：2-3天 | - | - | - |
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| 源叶(MedMol) | S87543-50mg | 98% | ￥1100.00元 | 预计交期：2-3天 | - | - | - |
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| 源叶(MedMol) | S87543-100mg | 98% | ￥1800.00元 | 预计交期：2-3天 | - | - | - |
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| 产品描述： PF-04217903 mesylate is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 mesylate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties | ||||||||||||||||||||
| 靶点： Ki: 4.8 nM (human c-Met);c-Met/HGFR | ||||||||||||||||||||
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体外研究： PF-04217903 mesylate (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[1].PF-04217903 mesylate induces apoptosis of GTL-16 cells (IC50=31 nM) . PF-04217903 mesylate 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 mesylate 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, but has no inhibitory activity against c-Met-Y1230C with IC50 of >10 μM. Cell Proliferation Assay Cell Line: GTL-16, H1993 cells Concentration: 0.1, 1, 10, 100, 1000, 10000 nM Incubation Time: 48-72 hours Result: Inhibited proliferation of c-Met–amplified human GTL-16 gastric carcinoma and H1993 NSCLC cells with IC50 values of 12 and 30 nM, respectively. Apoptosis Analysis Cell Line: GTL-16 cells Concentration: 1.5-3333 nM Incubation Time: 48 hours Result: Induced apoptosis of GTL-16 cells (IC50=31 nM). |
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体内研究： PF-04217903 mesylate (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 mesylate (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 mesylate 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 mesylate 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. |
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参考文献： 1. Timofeevski SL, et al. Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors. Biochemistry, 2009, 48(23), 5339-5349. 2. Shojaei F, et al. HGF/c-Met acts as an alternative angiogenic pathway in sunitinib-resistant tumors. Cancer Res, 2010, 70(24), 10090-10100. 3. Krumbach R, et al. Primary resistance to cetuximab in a panel of patient-derived tumour xenograft models: activation of MET as one mechanism for drug resistance. Eur J Cancer, 2011, 47(8), 1231-1243. |
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| 溶解性： Soluble in DMSO | ||||||||||||||||||||
| 保存条件： -20℃ | ||||||||||||||||||||
配置溶液浓度参考：
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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