Golvatinib (Synonyms: E-7050)

目录号: HY-13068 纯度: 99.89%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

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

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Golvatinib Chemical Structure

CAS No. : 928037-13-2

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10 mM * 1 mL in DMSO	￥980	In-stock
5 mg	￥700	In-stock
10 mg	￥1100	In-stock
50 mg	￥3800	In-stock
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Customer Review

MCE 顾客使用本产品发表的 4 篇科研文献

: Golvatinib purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]; Immunoblot analysis in MV-4-11 cells and MOLM-13, FLT3-WT and FLT3-ITD transfected HEK293 cells, and Ba/F3 FLT3-ITD cells revealed FLT3 target engagement for Golvatinib and Cabozantinib.

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC₅₀s of 14 and 16 nM, respectively.

IC₅₀ & Target^[1]

VEGFR2

16 nM (IC₅₀)

c-Met

14 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	6.89 μM Compound: 3	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32173195]
A549	IC₅₀	7.7 μM Compound: 1	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 33316412]
EBC-1	IC₅₀	6.2 nM Compound: E7050; Golvatinib	Cytotoxicity against human EBC1 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay Cytotoxicity against human EBC1 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay	[PMID: 26717201]
HeLa	IC₅₀	4.14 μM Compound: 3	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32173195]
HeLa	IC₅₀	4.23 μM Compound: 1	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 33316412]
HepG2	IC₅₀	65.5 μM Compound: Golvatinib	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 25082515]
Hs746T	IC₅₀	23 nM Compound: E7050; Golvatinib	Cytotoxicity against human Hs 746T cells assessed as inhibition of tumour growth after 3 days by WST-8 assay Cytotoxicity against human Hs 746T cells assessed as inhibition of tumour growth after 3 days by WST-8 assay	[PMID: 26717201]
HUVEC	IC₅₀	> 1000 nM Compound: E7050; Golvatinib	Antiangiogenic activity in HUVEC assessed as inhibition of bFGF induced cell proliferation after 3 days by WST-1 assay Antiangiogenic activity in HUVEC assessed as inhibition of bFGF induced cell proliferation after 3 days by WST-1 assay	[PMID: 26717201]
HUVEC	IC₅₀	16 nM Compound: E7050; Golvatinib	Inhibition of VEGFR-2 autophosphorylation in HUVEC after 1 hr by Western blot analysis Inhibition of VEGFR-2 autophosphorylation in HUVEC after 1 hr by Western blot analysis	[PMID: 26717201]
HUVEC	IC₅₀	16 nM Compound: 15; E7050	Inhibition of VEGF induced VEGFR2 phosphorylation in HUVEC preincubated for 1 hr followed by VEGF-stimulation for 5 mins by Western blot analysis Inhibition of VEGF induced VEGFR2 phosphorylation in HUVEC preincubated for 1 hr followed by VEGF-stimulation for 5 mins by Western blot analysis	[PMID: 27299736]
HUVEC	IC₅₀	17 nM Compound: E7050; Golvatinib	Antiangiogenic activity in HUVEC assessed as inhibition of HGF induced cell proliferation after 3 days by WST-1 assay Antiangiogenic activity in HUVEC assessed as inhibition of HGF induced cell proliferation after 3 days by WST-1 assay	[PMID: 26717201]
HUVEC	IC₅₀	84 nM Compound: E7050; Golvatinib	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF induced cell proliferation after 3 days by WST-1 assay Antiangiogenic activity in HUVEC assessed as inhibition of VEGF induced cell proliferation after 3 days by WST-1 assay	[PMID: 26717201]
MCF7	IC₅₀	15.44 μM Compound: 1	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 33316412]
MCF7	IC₅₀	20.61 μM Compound: 3	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32173195]
MCF7	IC₅₀	49.6 μM Compound: Golvatinib	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 25082515]
MKN-45	IC₅₀	14 nM Compound: 15; E7050	Inhibition of MET autophosphorylation in human MKN45 cells after 2 hrs by Western blot analysis Inhibition of MET autophosphorylation in human MKN45 cells after 2 hrs by Western blot analysis	[PMID: 27299736]
MKN-45	IC₅₀	14 nM Compound: E7050; Golvatinib	Inhibition of c-Met autophosphorylation in human MKN45 cells after 2 hrs by Western blot analysis Inhibition of c-Met autophosphorylation in human MKN45 cells after 2 hrs by Western blot analysis	[PMID: 26717201]
MKN-45	IC₅₀	37 nM Compound: E7050; Golvatinib	Cytotoxicity against human MKN45 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay Cytotoxicity against human MKN45 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay	[PMID: 26717201]
SNU-5	IC₅₀	24 nM Compound: E7050; Golvatinib	Cytotoxicity against human SNU5 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay Cytotoxicity against human SNU5 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay	[PMID: 26717201]

体外研究
(In Vitro)

Golvatinib (E-7050) 有效抑制 c-Met 和 VEGFR-2 的磷酸化。Golvatinib 还有效抑制 c-met 扩增的肿瘤细胞和用 HGF 或 VEGF 刺激的内皮细胞的生长。
Golvatinib 强烈抑制 MKN45、EBC-1、Hs746T 和 SNU-5 肿瘤细胞的生长， IC ₅₀ 值分别为 37、6.2、23 和 24 nM。Golvatinib 抑制 A549、SNU-1 和 0MKN74 肿瘤细胞的生长，具有更高的 IC₅₀ 值^[1]。
Golvatinib 避免了对所有在体外阻断 Met/Gab1/PI3K/Akt 通路，在 EGFR 突变肺癌细胞系中由外源性和/或内源性 HGF 诱导的可逆、不可逆和突变选择性 EGFR-TKIs。/br>Golvatinib 还可以防止因持续暴露于 HGF^[2] 而诱导的对吉非替尼具有耐药性的 HCC827 细胞的出现。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Golvatinib（E-7050）显示出对肿瘤内c-Met和VEGFR-2磷酸化的抑制作用，并在异种移植模型中表现出强烈的肿瘤生长抑制及肿瘤血管生成抑制作用。
针对含有c-met扩增的一些肿瘤细胞系，使用高剂量Golvatinib（50-200 mg/kg）治疗可导致肿瘤消退甚至消失。在一个腹膜扩散模型中，Golvatinib不仅对抗腹膜肿瘤有效，还显著延长了处理组小鼠的生存期^[1]。
Golvatinib（E7050）与吉非替尼联合使用能够明显抑制肿瘤生长，这与癌细胞中Akt磷酸化受到抑制相关^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

633.69

Formula

C₃₃H₃₇F₂N₇O₄

CAS 号

928037-13-2

性状

固体

颜色

White to off-white

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
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (78.90 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5781 mL	7.8903 mL	15.7806 mL
5 mM	0.3156 mL	1.5781 mL	3.1561 mL
10 mM	0.1578 mL	0.7890 mL	1.5781 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.28 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.28 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.28 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.89%

选择批次：

Data Sheet (646 KB) SDS (393 KB)

COA (259 KB) RP-HPLC (194 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

[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. [Content Brief]

Cell Assay ^[1]	Cells (1000-3000 cells/100 μL/well) are seeded on 96-well culture plates with various concentrations of Golvatinib and cultured for 3 days. Then, 10 μL of WST-8 reagent is added to each well, and absorbance is measured at 450 nm compared with a reference measurement at 660 nm using a MTP-500 microplate reader^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: Nude mice bearing MKN45, Hs746T, SNU-5, or EBC-1 tumors are administered Golvatinib (25, 50, 100, 200 mg/kg) or vehicle only as a control, once a day. Tumor volume is measured using calipers on the indicated days (0-15 days)^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief] [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. [Content Brief]

Golvatinib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5781 mL	7.8903 mL	15.7806 mL	39.4515 mL
	5 mM	0.3156 mL	1.5781 mL	3.1561 mL	7.8903 mL
	10 mM	0.1578 mL	0.7890 mL	1.5781 mL	3.9451 mL
	15 mM	0.1052 mL	0.5260 mL	1.0520 mL	2.6301 mL
	20 mM	0.0789 mL	0.3945 mL	0.7890 mL	1.9726 mL
	25 mM	0.0631 mL	0.3156 mL	0.6312 mL	1.5781 mL
	30 mM	0.0526 mL	0.2630 mL	0.5260 mL	1.3150 mL
	40 mM	0.0395 mL	0.1973 mL	0.3945 mL	0.9863 mL
	50 mM	0.0316 mL	0.1578 mL	0.3156 mL	0.7890 mL
	60 mM	0.0263 mL	0.1315 mL	0.2630 mL	0.6575 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Golvatinib928037-13-2E-7050E7050E 7050c-Met/HGFRVEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Golvatinib (Synonyms: E-7050)

Customer Review

MCE 顾客使用本产品发表的 4 篇科研文献