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Foretinib

(Synonyms: XL880; GSK1363089; GSK089; EXEL-2880)

目录号: PL01407 纯度: ≥99%

Foretinib是一种多靶点酪氨酸激酶抑制剂，抑制 Met 和 KDR 的IC50分别为0.4 nM 和 0.9 nM。

CAS No. :849217-64-7

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中文名称	Foretinib
中文别名	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;2-溴-1-(4-氟苯基)-1-丁酮;Foretinib (GSK1363089) 抑制剂;Foretinib标准品;N-[3-氟-4-[[6-甲氧基-7-[[3-(吗啉-4-基)丙基]氧]喹啉-4-基]氧];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;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	Foretinib
英文别名	N-(3-Fluoro-4-((6-methoxy-7-(3-morpholinopropoxy)quinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;Foretinib (GSK1363089);Foretinib;Foretinib (GSK1363089, GSK089, XL880,EXEL-2880);Foretinib (GSK1363089, XL880);GSK 1363089;N-(3-Fluoro-4-((6-methoxy-7-(3-morpholinopropoxy)quinolin-4-yl)-oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;XL880;4-(4-(o-Methoxyphenyl)piperazinyl)-1-(3,4,5-trimethoxyphenyl)-1-butanol dihydrochloride;4-(4-Hydroxy-4-(3,4,5-trimethoxyphenyl)butyl)-1-(o-methoxyphenyl)piperazine dihydrochloride;4-[4-(2-methoxyphenyl)piperazin-1-yl]-1-(3,4,5-trimethoxyphenyl)butan-1-ol dihydrochloride;EXEL-2880;GSK089;GSK136308;N1-{3-fluoro-4-[(6-(methyloxy)-7-{[3-(4-morpholinyl)propyl]oxy}-4-quinolinyl)oxy]phenyl}-N1'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide;XL-880,Foretinib;GSK1363089;XL 880;EXEL 2880;81FH7VK1C4;GSK1363089G;N-[3-Fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide;C34H34F2N4O6;88Z;n-(3-fluoro-4-((6-methoxy-7-(3-(4-morpholinyl)propoxy)-4-quinolinyl)oxy)phenyl)-n'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide;N-(3-Fluoro-4-{[6-Methoxy-7-(3-Morphol
Cas No.	849217-64-7
分子式	C₃₄H₃₄F₂N₄O₆
分子量	632.65
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	Foretinib是一种多靶点酪氨酸激酶抑制剂，抑制 Met 和 KDR 的IC50分别为0.4 nM 和 0.9 nM。

产品详情

Foretinib是一种多靶点酪氨酸激酶抑制剂，抑制 Met 和 KDR 的IC₅₀分别为0.4 nM 和 0.9 nM。

生物活性

Foretinib is a multi-target tyrosine kinase inhibitor with IC 50 s of 0.4 nM and 0.9 nM for Met and KDR.

性状

Solid

IC50 & Target[1][2]

KDR 0.9 nM (IC50) c-Met 0.4 nM (IC50

体外研究(In Vitro)

Foretinib inhibits HGF receptor family tyrosine kinases with IC50 values of 0.4 nM for Met and 3 nM for Ron. Foretinib also inhibits KDR, Flt-1, and Flt-4 with IC50 values of 0.9 nM, 6.8 nM and 2.8 nM, respectively. Foretinib inhibits colony growth of B16F10, A549 and HT29 cells with IC50 of 40 nM, 29 nM and 165 nM, respectively. A recent study indicates Foretinib affects cell growth differently in gastric cancer cell lines MKN-45 and KATO-III. Foretinib inhibits phosphorylation of MET and downstream signaling molecules in MKN-45 cells, while targets GFGR2 in KATO-III cells. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Foretinib (100 mg/kg, p.o.) 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 persist through 24 hours. Foretinib (30-100 mg/kg, once daily, p.o.) 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 Foretinib, respectively. Foretinib 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 Foretinib is well tolerated with no significant body weight loss. Foretinib is developed to target abnormal signaling of HGF through Met and simultaneously target several receptors tyrosine kinase involved in tumor angiogenesis. Foretinib causes tu

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Qian F, et al. Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases. Cancer Res, 2009, 69(20), 8009-8016.
[2]. Kataoka Y, et al. Foretinib (GSK1363089), a multi-kinase inhibitor of MET and VEGFRs, inhibits growth of gastric cancer cell lines by blocking inter-receptor tyrosine kinase networks. Invest New Drugs, 2011.

溶解度数据	In Vitro: DMSO : 75 mg/mL (118.55 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Foretinib

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