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    Tie2 kinase inhibitor
    Tie2 kinase inhibitor

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0632
    CAS #: 948557-43-5Purity ≥98%

    Description: Tie2 kinase inhibitor is novel, potent, reversible and selective ATP-competitive  Tie2 inhibitor with IC50 of 0.25 μM. It is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38. Tie2 kinase inhibitor exhibited significant inhibitory effect on Tie2 auto-phosphorylation and disrupted its downstream signal transduction in a dose dependent manner in human aortic endothelial cells. In addition, Tie2 kinase inhibitor exhibits moderately suppressed the activity of Tie2 tyrosine kinase in HEL cells with IC50 of 232 nM.

    References: Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60.

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    Molecular Weight (MW)439.53
    FormulaC26H21N3O2S
    CAS No.948557-43-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 35 mg/mL (79.6 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)2% Cremophor EL, 2% N,N-dimethylacetamide: 30 mg/mL
    Synonyms

    Synonym:  Tie2-inhibitor-5; Tie2 IN 5; Tie2IN5; Tie2 kinase inhibitor 5; Tie2-IN-5; Tie2 inhibitor 5;Compound 5;

    Chemical Name: 4-[4-(6-Methoxy-2-naphthalenyl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-5-yl]pyridine

    InChi Key: SINQIEAULQKUPD-UHFFFAOYSA-N

    InChi Code: InChI=1S/C26H21N3O2S/c1-31-22-8-5-19-15-21(4-3-20(19)16-22)25-24(17-11-13-27-14-12-17)28-26(29-25)18-6-9-23(10-7-18)32(2)30/h3-16H,1-2H3,(H,28,29)

    SMILES Code: O=S(C1=CC=C(C2=NC(C3=CC=C4C=C(OC)C=CC4=C3)=C(C5=CC=NC=C5)N2)C=C1)C


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    In Vitro

    In vitro activity: Tie2 kinase inhibitor exhibits a moderate inhibitory activity against Tie2 tyrosine kinase. Tie2 kinase inhibitor also shows moderate cellular activities with IC50 of 232 nM in HEL cells. Furthermore, Tie2 kinase inhibitor has a remarkable selectivity for Tie2 over p38 (IC50=50 μM) and a >10-fold selectivity over VEGFR2, VEGFR3, and PDGFR1β.


    Kinase Assay: Turned on an incubator shaker and adjusted temperature to 30 °C. Added 20 μL of 3× kinase buffer (final 20 mM Tris-HCl, pH 7, 100 mM NaCl, 12 mM MgCl2, 1 mM DTT) per well to the Flashplate. Added 20 μL of protein per well except for background. Added Tie2 Kinase Inhibitor, typically 1 ~ 2 μL in DMSO stocks. Added 20 μL of a mixture of gamma 33p-ATP and cold ATP (1:1 v/v) per well. Covered with transparent polyester film. Incubated at 30 °C for 2 hrs in shaker, washed five times. Read plate on TopCount or other counting instrument, and results were calculated as IC50 values using normal methods.


    Cell Assay: In HEL cells, Tie2 Kinase Inhibitor moderately suppressed the activity of Tie2 tyrosine kinase, with an IC50 value of 232 NM.

    In VivoIn a Matrigel mouse model of angiogenesis, Tie2 kinase inhibitor, at doses of 25 and 50 mg/kg (i.p., b.i.d), leads to a reduction of 41% and 70% of angiogenesis, respectively. In a MOPC-315 plasmacytoma xenograft model, Tie2 kinase inhibitor treatment results in a modest dose dependent delay in tumor growth.
    Animal modelMOPC-315 plasmacytoma xenograft model.
    Formulation & DosageDissolved in 5% EtOH+5%cremophor+90% water.; 50 mg/kg; i.p. injection
    References

    Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Tie2 kinase inhibitor

    Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60.

    Tie2 kinase inhibitor

    Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60.

    Tie2 kinase inhibitor

    Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60.


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