Cat. No. Name Size Price Add Cart
KI0420JNJ-388776052 mg$112
JNJ-388776055 mg$240
JNJ-3887760510 mg$432
JNJ-3887760550 mg$1232
JNJ-38877605100 mg$2032

Chemical Characteristic

Product NameJNJ-38877605
CAS No.943540-75-8
Molecular Weight 377.35
FormulaC19H13F2N7
Chemical Name6-(difluoro(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)quinoline
Smilesn1cccc2cc(ccc12)C(c1n2c(ccc(n2)c2cnn(c2)C)nn1)(F)F
Chemical Structure

Biological activities

JNJ-38877605 is a small-molecule, ATP-competitive inhibitor of the catalytic activity of c-Met. JNJ-38877605 displays ∼600-fold selectivity for c-Met compared with a panel of ∼250 diverse tyrosine and serine-threonine kinases and was found to potently inhibit HGF-stimulated and constitutively activated c-Met phosphorylation in vitro.[1] JNJ-38877605 inhibits c-Met Delfia autophosphorylation and c-Met phosphorylation with IC50 of 2 and 106 nM, in a kinase assay and a cell-based ELISA assay, respectively. JNJ-38877605 inhibits HepG2 cells with an IC50 of 0.3 nM in a scatter assay. JNJ-38877605 also has an effect on tumor regression in a S114 and U87MG tumor xenograft model.[2] Prevention of its kinase activity by treatment with JNJ-38877605 counteracts radiation-induced invasiveness. JNJ-38877605 promotes apoptosis. JNJ-38877605 prevents cells from resuming proliferation after irradiation in vitro. Treatment with MET inhibitors strengthens the efficacy of ionizing radiation (IR) to stop the growth of or to induce the regression of xenografts. [3] Treatment of mice with JNJ-38877605 for 72 hours leads to a markedly significant decrease in the plasma levels of human IL-8 (from ∼ 0.150 to 0.050 ng/mL) and GRO (from 0.080 to 0.030 ng/mL).[4]

References

[1] Eder JP, et al. Novel therapeutic inhibitors of the c-Met signaling pathway in cancer. Clin Cancer Res. 2009, 15(7): 2207-2214.
[2] Porter J. Small molecule c-Met kinase inhibitors: a review of recent patents. Expert Opin Ther Pat. 2010, 20(2): 159-177.
[3] De Bacco F, et al. Induction of MET by ionizing radiation and its role in radioresistance and invasive growth of cancer. J Natl Cancer Inst. 2011, 103(8): 645-661.
[4] Torti D, et al. A preclinical algorithm of soluble surrogate biomarkers that correlate with therapeutic inhibition of the MET oncogene in gastric tumors. Int J Cancer. 2012, 130(6): 1357-1366.

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