Golvatinib (E7050)
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Golvatinib是一种c-Met和VEGFR-2酪氨酸激酶的抑制剂,IC50值分别为14 nM和16 nM[1].
小分子化合物golvatinib是一种c-Met和VEGFR-2的双重抑制剂.它作为一种具有更强的抗肿瘤活性的治疗试剂被开发.Golvatinib抑制胃癌MKN45细胞c-Met的自磷酸化和人脐静脉内皮细胞(HUVECs)VEGFR-2的磷酸化,IC50值分别为14 nM和16 nM.Golvatinib也能抑制多种肿瘤细胞的生长,包括MKN45\EBC-1\Hs746T和SNU-5.除此之外,golvatinib有效抑制HGF或VEGF诱导的生长,IC50值为17 nM和84 nM[1].
在MKN45\Hs746T\SUN-5和EBC-1肿瘤细胞系异种移植小鼠模型上,golvatinib显著抑制肿瘤的生长.在VEGF过表达的人胰腺癌细胞系KP-1 /VEGF异种移植小鼠模型中,E7050单一给药,可减少VEGFR-2的磷酸化,随后通过抑制VEGF/VEGFR-2介导的肿瘤血管生成从而抑制肿瘤的生长[1].
参考文献:
[1] Nakagawa T, Tohyama O, Yamaguchi A, et al. E7050: A dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer science, 2010, 101(1): 210-215.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 633.69 |
Cas No. | 928037-13-2 |
Formula | C33H37F2N7O4 |
Solubility | insoluble in H2O; ≥1.39 mg/mL in EtOH with ultrasonic; ≥15.85 mg/mL in DMSO with gentle warming |
Chemical Name | 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 |
SDF | Download SDF |
Canonical SMILES | CN1CCN(CC1)C2CCN(CC2)C(=O)NC3=NC=CC(=C3)OC4=CC(=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | Golvatinib(E7050)是一种c-Met和VEGFR-2的双重抑制剂,IC50值分别为14 nM和16 nM. | |||||
靶点 | c-Met | VEGFR2 | ||||
IC50 | 14 nM | 16 nM |
化学结构
![Golvatinib (E7050)](http://www.apexbt.com//media/diy/images/struct/B1439.png)