Ki8751

This product is for research use only, not for human use. We do not sell to patients.

Ki8751
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Size Price Stock
500mg$650Check With Us
1g$1050Check With Us
5g$2660Check With Us

Cat #: V0502 CAS #: 228559-41-9 Purity ≥ 98%

Description: Ki8751 (Ki-8751), a quinolyloxyphenyl-urea analog, is a novel, cell-permeable and selective inhibitor of VEGFR2 (Flk-1) with potential anticancer activity.

References: Kubo K, et al. 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, 48(5), 1359-1366.

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Product Promise

Promise
Molecular Weight (MW)469.41
Molecular FormulaC24H18F3N3O4
CAS No.228559-41-9
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 47 mg/mL (100.1 mM)r
Water: <1 mg/mLr
Ethanol:<1 mg/mL
SMILES CodeO=C(NC1=CC=C(OC2=CC=NC3=CC(OC)=C(OC)C=C23)C=C1F)NC4=CC=C(F)C=C4F
SynonymsKi-8751; Ki 8751; Ki8751
ProtocolIn VitroKi8751 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.
In VivoKi8751 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.1303 mL10.6517 mL21.3033 mL42.6067 mL
5mM0.4261 mL2.1303 mL4.2607 mL8.5213 mL
10mM0.2130 mL1.0652 mL2.1303 mL4.2607 mL
20mM0.1065 mL0.5326 mL1.0652 mL2.1303 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.