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KI8751

  Cat. No.:  DC7440   Featured
Chemical Structure
228559-41-9
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More than 5000 active chemicals with high quality for research!
Field of application
Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 228559-41-9
Chemical Name: 1-(2,4-Difluorophenyl)-3-(4-(6,7-dimethoxyquinolin-4-yloxy)-2-fluorophenyl)urea
Synonyms: Ki8751;1-(2,4-difluorophenyl)-3-(4-(6,7-diMethoxyquinolin-4-yloxy)-2-fluorophenyl)urea;1-(2,4-difluorophenyl)-3-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-fluorophenyl]urea;Ki-8751;Ki-8751,Ki8751;N-(2,4-Difluorophenyl)-N'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-fluorophenyl]urea;Ki 8751;C24H18F3N3O4;1-(2,4-difluorophenyl)-3-(4-((6,7-dimethoxyquinolin-4-yl)oxy)-2-fluorophenyl)urea;1-(2,4-difluorophenyl)-3-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-2-fluorophenyl}urea;MLS006011284;KS-0
SMILES: FC1C([H])=C(C([H])=C([H])C=1N([H])C(N([H])C1C([H])=C([H])C(=C([H])C=1F)F)=O)OC1C([H])=C([H])N=C2C([H])=C(C(=C([H])C2=1)OC([H])([H])[H])OC([H])([H])[H]
Formula: C24H18F3N3O4
M.Wt: 469.4126
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Ki8751 is a potent VEGFR2 inhibitor with an IC50 of 0.9 nM.
In Vivo: Ki8751 shows 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 shows 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[1].
In Vitro: Ki8751 inhibits VEGFR-2 phosphorylation at an IC50 value of 0.90 nM, and also inhibits the PDGFR family members such as PDGFRR and c-Kit at 67 nM and 40 nM, respectively. However, Ki8751 does not have any inhibitory activity against other kinases such as EGFR, HGFR, InsulinR and others even at 10000 nM. Ki8751 suppresses the growth of the VEGF-stimulated human umbilical vein endothelial cell (HUVEC) on a nanomolar level[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC12371 XL-999(Tyrosine kinase-IN-1) XL999, a Spectrum Selective Kinase Inhibitor(TM) (SSKIs), is a potent inhibitor of key RTKs implicated in the development and maintenance of tumor vasculature and in the proliferation of some tumor cells.
DC1082 ZM306416 ZM306416 is a vascular endothelial growth factor receptor (VEGFR) antagonist.
DC1097 XL-184 (Cabozantinib,BMS907351) XL184 (Cabozantinib) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.
DC11268 VEGFR2 kinase inhibitor I(SU-5408) VEGFR2 kinase inhibitor I(SU-5408)is a potent, cell-permeable inhibitor of mouse VEGFR2 kinase (IC50 = 70 nM).
DC3134 Vandetanib (ZD6474) Vandetanib (Zactima, ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
DC9586 Telatinib Telatinib(Bay 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively.
DC12256 TAS-115 mesylate (TAS-115 methanesulfonate) TAS-115 mesylate is a potent VEGFR and c-Met/HGFR kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
DC3146 Sunitinib malate Sunitinib Malate (Sutent, SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.
DC9781 SU4312(NSC86429) SU4312(NSC86429) is a selective, cell-permeable inhibitor of VEGFR2 and PDGFR tyrosine kinases (IC50s = 0.8 and 19.4 μM, respectively).
DC7509 SU1498 SU1498 is a selective inhibitor of the VEGFR2; inhibits Flk-1with an IC50 of value of 700 nM.
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