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, 10 mM in DMSO;KI8751;KI 8751;KI-8751;VEGFR2 Kinase Inhibitor VI, Ki8751;VEGFR2 Kinase Inhibitor VI Ki8751 Ki-8751
- CBNumber:
- CB71074331
- Molecular Formula:
- C24H18F3N3O4
- Molecular Weight:
- 469.41
- MDL Number:
- MFCD09971092
- MOL File:
- 228559-41-9.mol
- MSDS File:
- SDS
| Product description | Number | Pack Size | Price |
| VEGFR2 Kinase Inhibitor VI, Ki8751 | 676484 | 5mg | $265 |
| Ki8751 ≥98% | 18004 | 5mg | $61 |
| Ki8751 ≥98% | 18004 | 10mg | $112 |
| Ki8751 ≥98% | 18004 | 25mg | $234 |
| Ki8751 ≥98% | 18004 | 50mg | $437 |
| More product size | |||
| 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. |
| InChI | 1S/C24H18F3N3O4/c1-32-22-11-15-20(12-23(22)33-2)28-8-7-21(15)34-14-4-6-19(17(27)10-14)30-24(31)29-18-5-3-13(25)9-16(18)26/h3-12H,1-2H3,(H2,29,30,31) |
| InChIKey | LFKQSJNCVRGFCC-UHFFFAOYSA-N |
| SMILES | Fc1c(ccc(c1)F)NC(=O)Nc2c(cc(cc2)Oc3c4c(ncc3)cc(c(c4)OC)OC)F |
| FDA UNII | RP6UGT29FF |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
Ki8751 price More Price(35)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | 676484 | VEGFR2 Kinase Inhibitor VI, Ki8751 | 228559-41-9 | 5mg | $265 | 2025-07-31 | Buy |
| Cayman Chemical | 18004 | Ki8751 ≥98% | 228559-41-9 | 5mg | $61 | 2024-03-01 | Buy |
| Cayman Chemical | 18004 | Ki8751 ≥98% | 228559-41-9 | 10mg | $112 | 2024-03-01 | Buy |
| Cayman Chemical | 18004 | Ki8751 ≥98% | 228559-41-9 | 25mg | $234 | 2024-03-01 | Buy |
| Cayman Chemical | 18004 | Ki8751 ≥98% | 228559-41-9 | 50mg | $437 | 2024-03-01 | Buy |
Ki8751 Chemical Properties,Uses,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
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.
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.
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
[1] KAZUO KUBO. 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]. Journal of Medicinal Chemistry, 2005, 48 5: 1359-1366. DOI:10.1021/jm030427r
[2] PIETER VRIJENS. Influenza virus entry via the GM3 ganglioside-mediated platelet-derived growth factor receptor β signalling pathway.[J]. The Journal of general virology, 2019: 583-601. DOI:10.1099/jgv.0.001235
Ki8751 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29830 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49977 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32470 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 18884 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471; | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
| Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +8615965530500 | nickzhang@hangyubiotech.com | China | 8497 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 |
