An inhibitor of Met kinase
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JNJ-38877605

Item No. 27650

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[difluoro[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]-quinoline
CAS Number
943540-75-8
Molecular Formula
C19H13F2N7
Formula Weight
377.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Chloroform: 30 mg/ml
λmax
227, 253, 302 nm
SMILES
FC(C1=NN=C2N1N=C(C3=CN(C)N=C3)C=C2)(F)C4=CC5=C(C=C4)N=CC=C5
InChi Code
InChI=1S/C19H13F2N7/c1-27-11-13(10-23-27)16-6-7-17-24-25-18(28(17)26-16)19(20,21)14-4-5-15-12(9-14)3-2-8-22-15/h2-11H,1H3
InChi Key
JRWCBEOAFGHNNU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $95

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    10 mg

    $158

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    50 mg

    $510

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    100 mg

    $922

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    Product Description

    JNJ-38877605 is an ATP-competitive inhibitor of Met kinase (IC50 = 4 nM).1 It is at least 600-fold selective for Met in a panel of approximately 250 tyrosine and serine-threonine kinases. JNJ-38877605 inhibits the growth of cancer cell lines with MET gene amplification (IC50s = 11-50 nM) but has no effect on the growth of control cells with normal MET gene copy number or no MET expression.2 The efficacy of JNJ-38877605 against MET-amplified cells decreases in the presence of increasing concentrations of recombinant human hepatocyte growth factor (HGF). JNJ-38877605 (50 mg/kg) sensitizes tumors to radiotherapy in U251 glioma and MDA-MB-231 breast cancer mouse xenograft models and increases apoptosis in irradiated tumors in the MDA-MB-231 mouse xenograft model.3 It reduces tumor size by 6-fold and the number of blood vessels in tumors by 80% in an RU-P melanoma mouse xenograft model when administered at a dose of 20 mg/kg.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Perera, T., Lavrijssen, T., Janssens, B., et al. JNJ-38877605: A selective Met kinase inhibitor inducing regression of Met-driven tumor models. Cancer Res. 68(9Supp.), (2008).

    2. Pennacchietti, S., Cazzanti, M., Bertotti, A., et al. Microenvironment-derived HGF overcomes genetically determined sensitivity to anti-MET drugs. Cancer Res. 74(22), 6598-6609 (2014).

    3. De Bacco, F., Luraghi, P., Medico, E., et al. Induction of MET by ionizing radiation and its role in radioresistance and invasive growth of cancer. J. Natl. Cancer Inst. 103(8), 645-661 (2011).

    4. Etnyre, D., Stone, A.L., Fong, J.T., et al. Targeting c-Met in melanoma: Mechanism of resistance and efficacy of novel combinatorial inhibitor therapy. Cancer Biol. Ther. 15(9), 1129-1141 (2014).