Ki8751
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
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.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ki8751是VEGFR-2有效的、选择性抑制剂,IC50值0.9 nM[1]。
VEGF受体是血管内皮生长因子(VEGF)的受体,可调节血管生成[2]。
在细胞实验中,Ki8751抑制VEGFR2的IC50值为0.9 nM。它也可抑制c-Kit(IC50值为40 nM)、PDGFRα(IC50 值为67 nM)和FGFR-2(IC50值为170 nM)[1]。用Ki8751(0.01、0.1、1、10、100 nM)以剂量依赖的方式处理人类脐静脉内皮细胞(HUVECs)导致HUVEC生长的抑制,Ki8751浓度为1 nM可完全抑制HUVEC的生长[1]。在MIP、RKO、SW620和SW480的转移性结直肠癌(CRC)细胞中,Ki8751(10 nM)诱导细胞衰老[2]。
人类神经胶质瘤GL07、人类胃癌ST-4、人类肺癌LC-6、人类结肠癌DLD-1和人黑色素瘤A375细胞的移植瘤裸鼠中,Ki8751抑制肿瘤的生长。人类肺癌LC-6的移植瘤裸鼠中,Ki8751首先抑制肿瘤的生长,然后又观察到肿瘤的再生[1]。
参考文献:
[1]. Kubo K, Shimizu T, Ohyama S, et al. Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas. J Med Chem, 2005, 48(5): 1359-1366.
[2]. Hasan MR, Ho SH, Owen DA, et al. Inhibition of VEGF induces cellular senescence in colorectal cancer cells. Int J Cancer, 2011, 129(9): 2115–2123.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 469.41 |
Cas No. | 228559-41-9 |
Formula | C24H18F3N3O4 |
Solubility | ≥23.45 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | 1-(2,4-difluorophenyl)-3-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-fluorophenyl]urea |
SDF | Download SDF |
Canonical SMILES | COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC(=C(C=C3)NC(=O)NC4=C(C=C(C=C4)F)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。 |
描述 | Ki8751是VEGFR-2酪氨酸激酶有效的选择性抑制剂,IC50值0.9 nM。 | |||||
靶点 | VEGFR-2 | |||||
IC50 | 0.9 nM |
质量控制和MSDS
- 批次:
化学结构
![Ki8751](http://www.apexbt.com//media/diy/images/struct/A1821.png)