Ki8751
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406351

CAS#: 228559-41-9

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).


Chemical Structure

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Ki8751
CAS# 228559-41-9

Theoretical Analysis

MedKoo Cat#: 406351
Name: Ki8751
CAS#: 228559-41-9
Chemical Formula: C24H18F3N3O4
Exact Mass: 469.12494
Molecular Weight: 469.41
Elemental Analysis: C, 61.41; H, 3.87; F, 12.14; N, 8.95; O, 13.63

Price and Availability

Size Price Availability Quantity
25.0mg USD 90.0 2 Weeks
50.0mg USD 150.0 2 Weeks
100.0mg USD 250.0 2 Weeks
200.0mg USD 450.0 2 Weeks
500.0mg USD 650.0 2 Weeks
1.0g USD 1150.0 2 Weeks
2.0g USD 1850.0 2 Weeks
5.0g USD 2950.0 2 Weeks
10.0g USD 4250.0 2 Weeks
Click to view more sizes and prices
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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

Appearance: White to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs

Storage Condition: 0 – 4 C for short term (weeks to 1 month) or -20 C for long terms (months to years).

Solubility: Soluble in DMSO, not soluble in water.

Shelf Life: >2 years if stored properly.

Drug Formulation: This drug may be formulated in DMSO.

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.03.00

Preparing Stock Solutions

The following data is based on the product molecular weight 469.41 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Pan Z, Fukuoka S, Karagianni N, Guaiquil VH, Rosenblatt MI. Vascular endothelial growth factor promotes anatomical and functional recovery of injured peripheral nerves in the avascular cornea. FASEB J. 2013 Jul;27(7):2756-67. doi: 10.1096/fj.12-225185. Epub 2013 Apr 8. PubMed PMID: 23568776; PubMed Central PMCID: PMC3688738.

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

3: Akiyama K, Ohga N, Hida Y, Kawamoto T, Sadamoto Y, Ishikawa S, Maishi N, Akino T, Kondoh M, Matsuda A, Inoue N, Shindoh M, Hida K. Tumor endothelial cells acquire drug resistance by MDR1 up-regulation via VEGF signaling in tumor microenvironment. Am J Pathol. 2012 Mar;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 drug resistance to vascular endothelial growth factor receptor 2 tyrosine kinase 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 cellular senescence in colorectal cancer cells. Int J Cancer. 2011 Nov 1;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 of follicle-stimulating hormone (FSH) and transforming growth factor (TGFβ1) in the regulation of ovarian angiogenesis. J Cell Physiol. 2011 Jun;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, Hasegawa K, Kobayashi Y, Takahashi N, Takahashi K, Kato S, Izawa T, Isoe T. 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 Mar 10;48(5):1359-66. PubMed PMID: 15743179.

Ki8751

25.0mg / USD 90.0


Additional Information