Golvatinib (E7050)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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
