| 公司名称： |
青岛凯亚隆化学有限公司 |
| 联系电话： |
+86-532-88191853 18254207708 |
| 产品介绍： |
中文名称:N-[3-氟-4-[[6-甲氧基-7-[[3-(吗啉-4-基)丙基]氧]喹啉-4-基]氧]苯基]-N'-(4-氟苯基)环丙烷-1,1-二甲酰胺
英文名称:GSK 1363089
CAS:849217-64-7
纯度：>98%HPLC white powder in stock 包装信息：100Mg;1g;5g;More 备注：现货 |
| 公司名称： |
长春吉大天元化学技术股份有限公司 |
| 联系电话： |
0431-85188877-804 |
| 产品介绍： |
英文名称:GSK 1363089
CAS:849217-64-7
纯度：2mg 备注：试剂级 |
| 公司名称： |
上海波以尔化工有限公司 |
| 联系电话： |
Mr Qiu 86-21-50182298(Domestic Market)Miss Xu 86-21-50180596(Abroad Market) |
| 产品介绍： |
中文名称:N-[3-氟-4-[[6-甲氧基-7-[[3-(吗啉-4-基)丙基]氧]喹啉-4-基]氧]苯基]-N'-(4-氟苯基)环丙烷-1,1-二甲酰胺
英文名称:GSK 1363089
CAS:849217-64-7
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| 公司名称： |
上海佰世凯化学科技有限公司 |
| 联系电话： |
+86(0)21-20908456 |
| 产品介绍： |
英文名称:Foretinib (GSK1363089, XL880)
CAS:849217-64-7
备注：C13684 |
| 公司名称： |
上海永璨生物科技有限公司 |
| 联系电话： |
0086-27-5925 3327; QQ:40199614 |
| 产品介绍： |
英文名称:Foretinib (GSK1363089, XL880)
CAS:849217-64-7
纯度：98% 包装信息：1g,5g,10g,50g 备注：only used for research |
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| 中文名称: | Foretinib (GSK1363089) | | 中文同义词: | N-[3-氟-4-[[6-甲氧基-7-[[3-(吗啉-4-基)丙基]氧]喹啉-4-基]氧]苯基]-N'-(4-氟苯基)环丙烷-1,1-二甲酰胺;FORETINIB GLAXOSMITHKLINE PAPILLARY RENAL CELL CARCINOMA PHASE IIRSCH. TRIANGLE PARK, NC (SEE ALSO HEAD/NECK) (888) 825-5249;GSK1363089; FORETINIB; EXEL-2880 | | 英文名称: | Foretinib (GSK1363089) | | 英文同义词: | Foretinib;GSK 1363089;EXEL-2880;XL880;N-[3-Fluoro-4-[[6-(methyloxy)-7-[[3-(morpholin-4-yl)propyl]oxy]quinolin-4-yl]oxy]phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;N-[3-Fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide;XL880(GSK1363089);foretinib
N1-{3-fluoro-4-[(6-(Methyloxy)-7-{[3-(4-Morpholinyl)propyl]oxy}-4-quinolinyl)oxy]phenyl}-N1'-(4-fluorophenyl)-1,1-cyclopropanedicarboxaMide | | CAS号: | 849217-64-7 | | 分子式: | C34H34F2N4O6 | | 分子量: | 632.6537664 | | EINECS号: | | | 相关类别: | 抗肿瘤药物;信号转导通路激酶抑制剂;医药中间体 |
| | Foretinib (GSK1363089) 性质 |
| 生物活性 | Foretinib (GSK1363089)是一种ATP竞争性的HGFR和VEGFR抑制剂，作用于Met和KDR作用最强，IC50分别为0.4 nM和0.9 nM，对Ron， Flt-1/3/4， Kit， PDGFRα/β和Tie-2作用效果稍弱，对FGFR1和EGFR几乎没有抑制活性。Phase 2。 | | 体外研究 | XL880 inhibits HGF receptor family tyrosine kinases with IC50 values of 0.4 nM for Met and 3 nM for Ron. XL880 also inhibits KDR, Flt-1, and Flt-4 with IC50 values of 0.9 nM, 6.8 nM and 2.8 nM, respectively. XL880 inhibits colony growth of B16F10, A549 and HT29 cells with IC50 of 40 nM, 29 nM and 165 nM, respectively. A recent study indicates XL880 affects cell growth differently in gastric cancer cell lines MKN-45 and KATO-III. XL880 inhibits phosphorylation of MET and downstream signaling molecules in MKN-45 cells, while targets GFGR2 in KATO-III cells. | | 体内研究 | A single 100 mg/kg oral gavage dose of XL880 results in substantial inhibition of phosphorylation of B16F10 tumor Met and ligand (e.g., HGFor VEGF)-induced receptor phosphorylation of Met in liver and Flk-1/KDR in lung, which both persisted through 24 hours. Treatment with XL880 (30-100 mg/kg, once daily, oral gavage) results in reduction in tumor burden. The lung surface tumor burden is reduced by 50% and 58% following treatment with 30 and 100 mg/kg XL880, respectively. XL880 treatment of mice bearing B16F10 solid tumors also results in dose-dependent tumor growth inhibition of 64% and 87% at 30 and 100 mg/kg, respectively. For both studies, administration of XL880 is well tolerated with no significant body weight loss. XL880 is developed to target abnormal signaling of HGF through Met and simultaneously target several receptors tyrosine kinase involved in tumor angiogenesis. XL880 caused tumor hemorrhage and necrosis in human xenografts within 2 to 4 hours, and maximal tumornecrosis is observed at 96 hours (after five daily doses), resulting in complete regression. |
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