Ki8751
- Product Name
- Ki8751
- CAS No.
- 228559-41-9
- Chemical Name
- Ki8751
- Synonyms
- Ki8751;CS-532;Ki8751, >=98%;Ki8751 hydrate;KI 8751; KI-8751;Ki8751 USP/EP/BP;KI8751;KI 8751;KI-8751;VEGFR2 Kinase Inhibitor VI, Ki8751;VEGFR2 Kinase Inhibitor VI Ki8751 Ki-8751;VEGFR2 Kinase Inhibitor VI, Ki8751 - CAS 228559-41-9 - Calbiochem
- CBNumber
- CB71074331
- Molecular Formula
- C24H18F3N3O4
- Formula Weight
- 469.41
- MOL File
- 228559-41-9.mol
Ki8751 Property
- Melting point:
- 239℃
- Density
- 1.429
- storage temp.
- −20°C
- solubility
- Soluble in DMSO (15 mg/ml)
- form
- Off-white solid
- color
- White
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
N-Bromosuccinimide Price
- Product number
- 676484
- Product name
- VEGFR2 Kinase Inhibitor VI, Ki8751
- Packaging
- 5mg
- Price
- $303
- Updated
- 2024/03/01
- Product number
- 18004
- Product name
- Ki8751
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $61
- Updated
- 2024/03/01
- Product number
- 18004
- Product name
- Ki8751
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $112
- Updated
- 2024/03/01
- Product number
- 18004
- Product name
- Ki8751
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $234
- Updated
- 2024/03/01
- Product number
- 18004
- Product name
- Ki8751
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $437
- Updated
- 2024/03/01
Ki8751 Chemical Properties,Usage,Production
Description
Ki8751 (228559-41-9) is a very potent (IC50 = 0.9 nM) inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2).1 It also inhibited PDGFRα (IC50 = 67 nM), c-Kit (IC50 = 40 nM), and FGFR2 (IC50 = 170 nM). Ki8751 completely suppressed HUVEC growth at 1 nM. Ki8751 completely inhibited tumor growth in LC-6 human tumor xenografts @ 5mg/kg. Ki8751 displayed anti-influenza A and B activity via disruption of virus entry in a PDGFR?/GM3-dependent manner.2
Uses
Ki8751 is a potent and selective inhibitor of VEGFR2, PDGFRα and c-Kit with IC50 of 0.9 nM, 67 nM and 40 nM, respectively.
Uses
KI 8751 is a potent and selective inhibitor of VEGFR-2-tyrosine kinase which inhibits proliferation of human umbilical vein endothelial cells and inhibits tumor growth.
Definition
ChEBI: 1-(2,4-difluorophenyl)-3-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-fluorophenyl]urea is an aromatic ether.
General Description
A cell-permeable quinolyloxyphenyl-urea compound that acts as a VEGFR-2-selective inhibitior in both cell-based (IC50 = 0.9 nM in VEGF-induced receptor phosphorylation) and cell-free (IC50 = 4.0 nM in kinase reactions) assays. It inhibits c-Kit, PDGFRα, and FGFR-2 only at much higher concentrations (IC50 = 40, 67, and 170 nM, respectively, in cell-based assays), while exhibiting no effect against eight other commonly studied receptor and non-receptor kinases even at concentrations as high as 10 μM. Effectively blocks VEGF-dependent, but not VEGF-independent, cell proliferation in vitro and tumor growth in mice and rats (5 to 20 mg/kg, daily p.o.) in vivo.
Biological Activity
Potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC 50 = 0.9 nM). Displays some inhibitory activity towards c-Kit, PDGFR α and FGFR-2 (IC 50 values range from 40 to 170 nM) but is highly selective over other receptor tyrosine kinases (IC 50 > 10000 nM for FGFR-2, EGFR and HGFR). Inhibits VEGF-stimulated proliferation of human umbilical vein endothelial cells (HUVEC) and inhibits tumor growth in vivo ; antiangiogenic.
storage
Store at +4°C
References
Kubo et al. (2005), 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. 48 1359 Vrijens et al. (2019), Influenza virus entry via the GM3 ganglioside-mediated platelet-derived growth factor receptor b signaling pathway; J. Gen. Virol. 100 583
Ki8751 Preparation Products And Raw materials
Raw materials
Preparation Products
Ki8751 Suppliers
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View Lastest Price from Ki8751 manufacturers
- Product
- Ki8751 228559-41-9
- Price
- US $7.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- JD 524
- Release date
- 2019-09-01