Ki8751

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WARNING: This product is for research use only, not for human or veterinary use.

Description:Ki8751 is a potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC50 = 0.9 nM). Displays some inhibitory activity towards c-Kit, PDGFR α and FGFR-2 (IC50 values range from 40 to 170 nM).

Price and Availability

Ki8751, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406351Name: Ki8751CAS#: 228559-41-9Chemical Formula: C24H18F3N3O4Exact Mass: 469.12494Molecular Weight: 469.41Elemental Analysis: C, 61.41; H, 3.87; F, 12.14; N, 8.95; O, 13.63

Synonym:Ki8751; Ki-8751; Ki 8751

IUPAC/Chemical Name:1-(2,4-difluorophenyl)-3-(4-((6,7-dimethoxyquinolin-4-yl)oxy)-2-fluorophenyl)urea

InChi Key:LFKQSJNCVRGFCC-UHFFFAOYSA-N

InChi Code: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)

SMILES Code:O=C(NC1=CC=C(OC2=CC=NC3=CC(OC)=C(OC)C=C23)C=C1F)NC4=CC=C(F)C=C4F

Technical Data

Additional Information

References

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2: Xu C, Wu X, Zhu J. VEGF promotes proliferation of human glioblastomamultiforme stem-like cells through VEGF receptor 2.ScientificWorldJournal. 2013;2013:417413. doi: 10.1155/2013/417413. Epub2013 Feb 28. PubMed PMID: 23533349; PubMed Central PMCID: PMC3603324.

3: Akiyama K, Ohga N, Hida Y, Kawamoto T, Sadamoto Y, Ishikawa S, MaishiN, Akino T, Kondoh M, Matsuda A, Inoue N, Shindoh M, Hida K. Tumorendothelial cells acquire drug resistance by MDR1 up-regulation via VEGFsignaling in tumor microenvironment. Am J Pathol. 2012Mar;180(3):1283-93. doi: 10.1016/j.ajpath.2011.11.029. Epub 2012 Jan 13.PubMed PMID: 22245726.

4: Arao T, Matsumoto K, Furuta K, Kudo K, Kaneda H, Nagai T, Sakai K,Fujita Y, Tamura D, Aomatsu K, Koizumi F, Nishio K. Acquired drugresistance to vascular endothelial growth factor receptor 2 tyrosinekinase inhibitor in human vascular endothelial cells. Anticancer Res.2011 Sep;31(9):2787-96. PubMed PMID: 21868521.

5: Hasan MR, Ho SH, Owen DA, Tai IT. Inhibition of VEGF induces cellularsenescence in colorectal cancer cells. Int J Cancer. 2011 Nov1;129(9):2115-23. doi: 10.1002/ijc.26179. Epub 2011 Aug 3. PubMed PMID:21618508.

6: Kuo SW, Ke FC, Chang GD, Lee MT, Hwang JJ. Potential role offollicle-stimulating hormone (FSH) and transforming growth factor(TGFβ1) in the regulation of ovarian angiogenesis. J Cell Physiol. 2011Jun;226(6):1608-19. doi: 10.1002/jcp.22491. PubMed PMID: 20945379.

7: Kubo K, Shimizu T, Ohyama S, Murooka H, Iwai A, Nakamura K, HasegawaK, Kobayashi Y, Takahashi N, Takahashi K, Kato S, Izawa T, Isoe T. Novelpotent orally active selective VEGFR-2 tyrosine kinase inhibitors:synthesis, structure-activity relationships, and antitumor activities ofN-phenyl-N"-{4-(4-quinolyloxy)phenyl}ureas. J Med Chem. 2005 Mar10;48(5):1359-66. PubMed PMID: 15743179.