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Ki8751

Chemical Structure : Ki8751

CAS No.: 228559-41-9

Ki8751 (Ki 8751, Ki-8751)

Catalog No.: PC-42853Not For Human Use, Lab Use Only.

Ki8751 is a potent, selective and orally active VEGFR-2 inhibitor that inhibits VEGFR-2 phosphorylation with IC50 of 0.6 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Ki8751 is a potent, selective and orally active VEGFR-2 inhibitor that inhibits VEGFR-2 phosphorylation with IC50 of 0.6 nM.
Ki8751 also inhibits PDGFR family members such as PDGFRα and c-Kit at 67 nM and 40 nM, does not have any inhibitory activity against other kinases such as EGFR, HGFR, InsulinR (IC50>10 uM).
Ki8751  suppressed the growth of the VEGF-stimulated HUVEC on nanomolar level, shows significant antitumor activity against human tumor xenografts such as glioma, stomach carcinoma), lung carcinoma, colon carcinoma and melanoma in nude mice.

Physicochemical Properties

M.Wt 469.4126
Formula C24H18F3N3O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: ≥92mg/mL; Water: <1.2mg/mL; Ethanol: <1.2mg/mL

Chemical Name/SMILES

Urea, N-(2,4-difluorophenyl)-N'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-fluorophenyl]-

References

1. Kubo K, et al. J Med Chem. 2005 Mar 10;48(5):1359-66.

2. Arao T, et al. Anticancer Res. 2011 Sep;31(9):2787-96.

3. Hasan MR, et al. Int J Cancer. 2011 Nov 1;129(9):2115-23.

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