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MedKoo Cat#: 406351 | Name: Ki8751
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Description:

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

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

Ki8751
Ki8751
CAS#228559-41-9

Theoretical Analysis

MedKoo Cat#: 406351

Name: Ki8751

CAS#: 228559-41-9

Chemical Formula: C24H18F3N3O4

Exact Mass: 469.1249

Molecular Weight: 469.42

Elemental Analysis: C, 61.41; H, 3.87; F, 12.14; N, 8.95; O, 13.63

Price and Availability

Size Price Availability Quantity
50mg USD 250.00 2 Weeks
100mg USD 450.00 2 Weeks
200mg USD 750.00 2 Weeks
500mg USD 1,350.00 2 Weeks
1g USD 2,150.00 2 Weeks
2g USD 3,650.00 2 Weeks
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Related CAS #
No Data
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
More Info
        
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Ki8751 is a potent VEGFR2 inhibitor with an IC50 of 0.9 nM.
In vitro activity:
VEGF blockade by Ki8751 significantly reduced cancer cell proliferation, and enhanced breast cancer cell apoptosis. Mass spectrometric analyses revealed that Ki8751 treatment significantly upregulated the expression of mitochondrial proteins, suggesting the involvement of mitochondrial biogenesis. Reference: Cancer Biol Med. 2021 Feb 15;18(1):139-154. https://pubmed.ncbi.nlm.nih.gov/33628590/
In vivo activity:
6ab (Ki8751) showed significant antitumor activity against five human tumor xenografts such as GL07 (glioma), St-4 (stomach carcinoma), LC6 (lung carcinoma), DLD-1 (colon carcinoma) and A375 (melanoma) in nude mice and also showed complete tumor growth inhibition with the LC-6 xenograft in nude rats following oral administration once a day for 14 days at 5 mg/kg without any body weight loss. Reference: J Med Chem. 2005 Mar 10;48(5):1359-66.
Solvent mg/mL mM
Solubility
DMF 25.0 53.26
DMF:PBS (pH 7.2) (1:3) 0.3 0.53
DMSO 51.5 109.68
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 469.42 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
Formulation protocol:
1. Ni H, Guo M, Zhang X, Jiang L, Tan S, Yuan J, Cui H, Min Y, Zhang J, Schlisio S, Ma C, Liao W, Nister M, Chen C, Li S, Li N. VEGFR2 inhibition hampers breast cancer cell proliferation via enhanced mitochondrial biogenesis. Cancer Biol Med. 2021 Feb 15;18(1):139-154. doi: 10.20892/j.issn.2095-3941.2020.0151. PMID: 33628590; PMCID: PMC7877175. 2. 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. PMID: 21618508. 3. Lee Y, Kim SJ, Choo J, Heo G, Yoo JW, Jung Y, Rhee SH, Im E. miR-23a-3p is a Key Regulator of IL-17C-Induced Tumor Angiogenesis in Colorectal Cancer. Cells. 2020 Jun 1;9(6):1363. doi: 10.3390/cells9061363. PMID: 32492770; PMCID: PMC7348989. 4. 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. doi: 10.1021/jm030427r. PMID: 15743179.
In vitro protocol:
1. Ni H, Guo M, Zhang X, Jiang L, Tan S, Yuan J, Cui H, Min Y, Zhang J, Schlisio S, Ma C, Liao W, Nister M, Chen C, Li S, Li N. VEGFR2 inhibition hampers breast cancer cell proliferation via enhanced mitochondrial biogenesis. Cancer Biol Med. 2021 Feb 15;18(1):139-154. doi: 10.20892/j.issn.2095-3941.2020.0151. PMID: 33628590; PMCID: PMC7877175. 2. 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. PMID: 21618508.
In vivo protocol:
1. Lee Y, Kim SJ, Choo J, Heo G, Yoo JW, Jung Y, Rhee SH, Im E. miR-23a-3p is a Key Regulator of IL-17C-Induced Tumor Angiogenesis in Colorectal Cancer. Cells. 2020 Jun 1;9(6):1363. doi: 10.3390/cells9061363. PMID: 32492770; PMCID: PMC7348989. 2. 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. doi: 10.1021/jm030427r. PMID: 15743179.
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.