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    JNJ-38877605
    JNJ-38877605

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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 #: V0601
    CAS #: 943540-75-8Purity ≥98%

    Description: JNJ-38877605 (JNJ38877605) is an orally bioavailable small-molecule inhibitor of c-Met with potential antitumor activity. It inhibits c-Met with an IC50 of 4 nM and shows 600-fold selectivity for inhibiting c-Met over 200 other kinases. 

    References: J Natl Cancer Inst. 2011 Apr 20;103(8):645-61; Int J Cancer. 2012 Mar 15;130(6):1357-66.


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    Molecular Weight (MW)377.35
    FormulaC19H13F2N7
    CAS No.943540-75-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 37 mg/mL (98.1 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL 
    SynonymsJNJ38877605; JNJ 38877605; JNJ-38877605; 

    Chemical Name: 6-(difluoro(6-(1-methyl-1H-pyrazol-3-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)quinoline

    InChi Key: HUWHDIWESZXGII-UHFFFAOYSA-N

    InChi Code: InChI=1S/C19H13F2N7/c1-27-10-8-16(25-27)15-6-7-17-23-24-18(28(17)26-15)19(20,21)13-4-5-14-12(11-13)3-2-9-22-14/h2-11H,1H3

    SMILES Code: CN1N=C(C2=NN3C(C=C2)=NN=C3C(C4=CC=C5N=CC=CC5=C4)(F)F)C=C1


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    In Vitro

    In vitro activity: JNJ-38877605 shows more than 600-fold selectivity for c-Met compared with more than 200 other diverse tyrosine and serine-threonine kinases and also potently inhibits HGF-stimulated and constitutively activated c-Met phosphorylation in vitro. In EBC1, GTL16, NCI-H1993, and MKN45 cells, JNJ-38877605 (500 nM) leads to a significant reduction of phosphorylation of Met and RON, another key player in invasive growth. A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells.


    Kinase Assay: JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.


    Cell Assay: JNJ-38877605 shows more than 600-fold selectivity for c-Met compared with more than 200 other diverse tyrosine and serine-threonine kinases and also potently inhibits HGF-stimulated and constitutively activated c-Met phosphorylation in vitro. In EBC1, GTL16, NCI-H1993, and MKN45 cells, JNJ-38877605 (500 nM) leads to a significant reduction of phosphorylation of Met and RON, another key player in invasive growth. A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells.

    In VivoIn mice bearing established GTL16 xenografts, JNJ-38877605, dosed orally with 40 mg/kg/day for 72 hours, results in a statistically significant decrease in the plasma levels of human IL-8 (from 0.150 ng/mL to 0.050 ng/mL) and GROα (from 0.080 ng/mL to 0.030 ng/mL). While concentrations of uPAR in the blood become reduced to more than 50% at the same dose.
    Animal modelGTL16 cells are inoculated subcutaneously into the right posterior flank (or both right and left posterior flanks, for determination of uPAR and IL-6) of 6-week-old immunodeficient nu/nu female mice on Swiss CD1 background.
    Formulation & DosageDissolved in PBS; ≤40mg/kg; p.o.
    ReferencesJ Natl Cancer Inst. 2011 Apr 20;103(8):645-61; Int J Cancer. 2012 Mar 15;130(6):1357-66.


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

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