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).

Product information

CAS Number: 228559-41-9

Molecular Weight: 469.41

Formula: C24H18F3N3O4

Synonym:

Ki-8751

Ki 8751

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

Smiles: COC1=CC2=C(C=CN=C2C=C1OC)OC1=CC(F)=C(C=C1)NC(=O)NC1=CC=C(F)C=C1F

InChiKey: LFKQSJNCVRGFCC-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO: 47 mg/mL(100.12 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Ki8751 potently and selectively inhibits VEGFR2 with IC50 of 0.9 nM. Ki8751 also inhibits PDGFRα, c-Kit, and FGFR-2, with much higher IC50 values (40 nM–170 nM). Except for these several kinases, Ki8751 doesn't disturb other kinases, including HGFR, EGFR, and InsulinR, even at 10 μM. In human umbilical vein endothelial cells (HUVECs), Ki8751 (1 nM–100 nM) effectively decreases VEGF-stimulated cell proliferation and vasculature permeability. In metastatic colorectal cancer (CRC) cells MIP, RKO, SW620, and SW480, but not in HCT116, Ki8751 (10 nM) increases cellular senescence.

In Vivo:

In nude mice bearing human tumor xenografts of GL07, St-4, LC6, DLD-1, and A375 cells, Ki8751 (20 mg/kg) inhibits tumor growth. In nude rat xenograft models of LC-6 cells, Ki8751 (5 mg/kg) completely inhibits tumor growth without affecting body weight.

References:

1. Hasan MR, et al. Int J Cancer, 2011, 129(9), 2115–2123.
2. Tamura D, et al. Cancer Sci, 2010, 101(6), 1403-1408.
3. Kubo K, et al. J Med Chem, 2005, 48(5), 1359-1366.

Products are for research use only. Not for human use.