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SU11274 (PKI SU11274; PKI SU11274)

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SU11274 (PKI SU11274; PKI SU11274)
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500mg$1650Check With Us
1g$2475Check With Us

Cat #: V0592 CAS #: 658084-23-2 Purity ≥ 98%

Description: SU11274 (also called PKI-SU11274; PKI-SU-11274) is a novel, potent and selective Met inhibitor with potential antineoplastic activity.

References: Wang X, et al. Potent and selective inhibitors of the Met [hepatocyte growth factor/scatter factor (HGF/SF) receptor] tyrosine kinase block HGF/SF-induced tumor cell growth and invasion. Mol Cancer Ther, 2003, 2(11):1085-1092.

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Molecular Weight (MW)568.09
Molecular FormulaC28H30CIN5O4S
CAS No.658084-23-2
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 92 mg/mL (161.9 mM)r
Water: <1 mg/mLr
Ethanol: 2 mg/mL (3.5 mM)
Solubility In Vivo30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
SMILES CodeO=S(C1=CC2=C(NC(/C2=CC3=C(C)C(C(N4CCN(C)CC4)=O)=C(C)N3)=O)C=C1)(N(C5=CC=CC(Cl)=C5)C)=O
SynonymsSU-11274; PKI-SU11274; PKI SU11274; PKI-SU11274;SU 11274; SU11274;
ProtocolIn VitroSU11274 exhibits greater than 50-fold selectivity for Met versus Flk and more than 500 times selectivity versus other tyrosine kinases such as FGFR-1, c-src, PDGFbR, and EGFR. SU11274 inhibits the phosphorylation of key regulators of the PI3K pathway, including AKT, FKHR, or GSK3β. SU11274 treatment inhibits the growth of TPR-MET-transformed BaF3 cells in a dose-dependent manner with IC50 of < 3 μM in the absence of interleukin 3, without growth inhibition of BaF3 cells transformed by other oncogenic tyrosine kinases, including BCR-ABL, TEL-JAK2, TEL-ABL, and TEL-PDGFβR. In addition to cell growth, SU11274 treatment significantly inhibits the migration of BaF3. TPR-MET cells by 44.8% and 80% at 1 μM and 5 μM, respectively. SU11274 inhibits HGF-dependent phosphorylation of Met as well as HGF-dependent cell proliferation and motility with an IC50 of 1-1.5 μM. In H69 and H345 cells which have functional Met receptor, SU11274 inhibits the HGF-induced cell growth with IC50 of 3.4 μM and 6.5 μM, respectively. SU11274 induces G1 cell cycle arrest with cells in G1 phase increased from 42.4% to 70.6% at 5 μM, and induces caspase-dependent apoptosis by 24% at 1 μM.
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
1mM1.7603 mL8.8014 mL17.6028 mL35.2057 mL
5mM0.3521 mL1.7603 mL3.5206 mL7.0411 mL
10mM0.1760 mL0.8801 mL1.7603 mL3.5206 mL
20mM0.0880 mL0.4401 mL0.8801 mL1.7603 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
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.