Golvatinib|928037-13-2|(E-7050)-陌孚医药/Medlife

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Golvatinib (Synonyms: E-7050)

目录号: PL03164 纯度: ≥99%

CAS No. :928037-13-2

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中文名称	Golvatinib
中文别名	N-[2-氟-4-[[2-[[[4-(4-甲基哌嗪-1-基)哌啶-1-基]羰基]氨基]吡啶-4-基]氧基]苯基]-N'-(4-氟苯基)环丙烷-1,1-二甲酰胺;N-[2-氟-4-[[2-[[[4-(4-甲基哌嗪-1-基)哌啶-1-基]羰基]氨基]吡啶-4-基]氧基]苯基]-N-(4-氟苯基)环丙烷-1,1-二甲酰胺;美索巴莫D5;N-[2-氟-4-[[2-[[[4-(4-甲基哌嗪-1-基)哌啶-1-基]羰基]氨基]吡啶-4-基]氧基]苯基]-N''-(4-氟苯基)环丙烷-1,1-二甲酰胺
英文名称	Golvatinib
英文别名	E-7050;N-[2-Fluoro-4-[[2-[[[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl]amino]pyridin-4-yl]oxy]phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;Golvatinib (E7050);1-N'-[2-fluoro-4-[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyridin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;E7050;Golvatinib;Golvatinib (USAN);UNII-516Z3YP58E;516Z3YP58E;N-(2-fluoro-4-(2-(4-(4-methylpiperazin-1-yl)piperidine-1-carboxamido)pyridin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;Golvatinib [USAN:INN];N-(2-Fluoro-4-{[2-({[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl}amino)pyridin;Golvatinib tartrate;N-(2-Fluoro-4-{[2-({[4-(4-methylpiperazin-1-yl)piperidi;N-[2-Fluoro-4-[[2-[[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]amino]-4-pyridinyl]oxy]phenyl]-N′-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide (ACI);1-N′-[2-Fluoro-4-[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyridin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;E 7050;N-[2-Fluoro-4-[[2-[[[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl]amino]pyridin-4-yl]oxy]phenyl]-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Cas No.	928037-13-2
分子式	C₃₃H₃₇F₂N₇O₄
分子量	633.69
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Golvatinib (E-7050) 是 c-Met 和 VEGFR2 的双重抑制剂，IC₅₀值分别为14 和 16 nM。

生物活性

Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC 50 s of 14 and 16 nM, respectively.

性状

Solid

IC50 & Target[1][2]

VEGFR2 16 nM (IC50) c-Met 14 nM (IC50

体外研究(In Vitro)

Golvatinib (E-7050) potently inhibits phosphorylation of both c-Met and VEGFR-2. Golvatinib also potently represses the growth of both c-met amplified tumor cells and endothelial cells stimulated with either HGF or VEGF.
Golvatinib strongly inhibits the growth of MKN45, EBC-1, Hs746T, and SNU-5 tumor cells with IC50 values of 37, 6.2, 23, and 24 nM, respectively. The growth of A549, SNU-1 and 0MKN74 tumor cells is inhibited by Golvatinib with much higher IC50 values.
Golvatinib circumvents resistance to all of the reversible, irreversible, and mutant-selective EGFR-TKIs induced by exogenous and/or endogenous HGF in EGFR mutant lung cancer cell lines, by blocking the Met/Gab1/PI3K/Akt pathway in vitro .
Golvatinib also prevents the emergence of gefitinib-resistant HCC827 cells induced by continuous exposure to HGF.

体内研究(In Vivo)

Golvatinib (E-7050) shows inhibition of the phosphorylation of c-Met and VEGFR-2 in tumors, and strong inhibition of tumor growth and tumor angiogenesis in xenograft models.
Treatment of some tumor lines containing c-met amplifications with high doses of Golvatinib (50-200 mg/kg) induced tumor regression and disappearance. In a peritoneal dissemination model, Golvatinib shows an antitumor effect against peritoneal tumors as well as a significant prolongation of lifespan in treated mice.
Golvatinib (E7050) plus Gefitinib results in marked regression of tumor growth associated with inhibition of Akt phosphorylation in cancer cells. has not independently confirmed the accuracy of these methods. They are for reference only.

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]. Nakagawa T et al. E7050: a dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer Sci, 2010, 101(1), 210-215.
[2]. Wang W et al. Met kinase inhibitor E7050 reverses three different mechanisms of hepatocyte growth factor-induced tyrosine kinase inhibitor resistance in EGFR mutant lung cancer. Clin Cancer Res, 2012, 18(6), 1663-1671.

溶解度数据	In Vitro: DMSO : 50 mg/mL (78.90 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。

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