Toggle Nav

Ki8751

In stock
Catalog No.
A1821
VEGFR-2 inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$85.00
In stock
5mg
$45.00
In stock
25mg
$150.00
In stock
100mg
$470.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Ki8751 is a selective and potent inhibitor of VEGFR2 with IC50 value of 0.9 nM [1].
VEGF receptors are receptors for vascular endothelial growth factor (VEGF) and regulate angiogenesis [2].
In cell-based assays, Ki8751 inhibited VEGFR2 with IC50 value of 0.9 nM. And it also inhibited c-Kit (IC50 40 nM), PDGFRα(IC50 67 nM), and FGFR-2 (IC50 170 nM) [1]. Treatment human umbilical vein endothelial cells (HUVECs) with Ki8751 (0.01, 0.1, 1, 10, 100 nM) caused inhibition of HUVEC growth in a dose-dependent way and completely suppressed it at 1 nM [1]. In metastatic colorectal cancer (CRC) cells of MIP, RKO, SW620, and SW480, Ki8751 (10 nM) induced cellular senescence [2].
In nude mice using xenografts of human glioma GL07, human stomach carcinoma St-4, human lung carcinoma LC-6, human colon carcinoma DLD-1 and human melanoma A375 cells, Ki8751 inhibited tumor growth. In nude rats using LC-6 human tumor xenografts, Ki8751 inhibited tumor growth, but then tumor regrowth was observed [1].
References:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt469.41
Cas No.228559-41-9
FormulaC24H18F3N3O4
Solubility≥23.45mg/mL in DMSO
Chemical Name1-(2,4-difluorophenyl)-3-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-fluorophenyl]urea
SDFDownload SDF
Canonical SMILESCOC1=CC2=C(C=CN=C2C=C1OC)OC3=CC(=C(C=C3)NC(=O)NC4=C(C=C(C=C4)F)F)F
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description Ki8751 is a potent and selective inhibitor of VEGFR-2 tyrosine kinase with IC50 value of 0.9 nM.
Targets VEGFR-2          
IC50 0.9 nM          

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

Ki8751