c-Met inhibitor 1 - CAS 1357072-61-7
Catalog number: 1357072-61-7
Category: Inhibitor
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c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer.
c-Met inhibitor 1; c Met inhibitor 1
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1.Discovery of a new series of imidazo[1,2-a]pyridine compounds as selective c-Met inhibitors.
Liu TC1,2, Peng X3, Ma YC2, Ji YC3, Chen DQ2, Zheng MY2, Zhao DM1, Cheng MS1, Geng MY3, Shen JK2, Ai J3, Xiong B2. Acta Pharmacol Sin. 2016 Apr 4. doi: 10.1038/aps.2016.11. [Epub ahead of print]
AIM: Aberrant c-Met activation plays a critical role in cancer formation, progression and dissemination, as well as in development of resistance to anticancer drugs. Therefore, c-Met has emerged as an attractive target for cancer therapy. The aim of this study was to develop new c-Met inhibitors and elaborate the structure-activity relationships of identified inhibitors.
2.MET Exon 14 Mutations in Non-Small-Cell Lung Cancer Are Associated With Advanced Age and Stage-Dependent MET Genomic Amplification and c-Met Overexpression.
Awad MM1, Oxnard GR2, Jackman DM2, Savukoski DO2, Hall D2, Shivdasani P2, Heng JC2, Dahlberg SE2, Jänne PA2, Verma S2, Christensen J2, Hammerman PS2, Sholl LM2. J Clin Oncol. 2016 Mar 1;34(7):721-30. doi: 10.1200/JCO.2015.63.4600. Epub 2016 Jan 4.
PURPOSE: Non-small-cell lung cancers (NSCLCs) harboring mutations in MET exon 14 and its flanking introns may respond to c-Met inhibitors. We sought to describe the clinical, pathologic, and genomic characteristics of patients with cancer with MET exon 14 mutations.
3.Design, synthesis and biological evaluation of novel 4-phenoxy-6,7-disubstituted quinolines possessing (thio)semicarbazones as c-Met kinase inhibitors.
Zhai X1, Bao G2, Wang L2, Cheng M3, Zhao M2, Zhao S2, Zhou H2, Gong P4. Bioorg Med Chem. 2016 Mar 15;24(6):1331-45. doi: 10.1016/j.bmc.2016.02.003. Epub 2016 Feb 4.
In continuing our efforts to identify small molecules able to inhibit c-Met kinase, three series of novel 6,7-disubstituted-4-phenoxyquinoline derivatives (23a-w, 26a-d and 30a-d) bearing (thio)semicarbazone scaffold were designed, synthesized and evaluated for their cytotoxicity. The biological data revealed that most compounds exhibited moderate-to-excellent activity against HT-29, MKN-45, A549 cancer cell lines and relative poor potency toward MDA-MB-231 cell as well as hardly any cytotoxicity in normal PBL cell. Eleven compounds were further examined for their inhibitory activity against c-Met kinase and three compounds (23h, 23n and 26a) demonstrated good inhibitory activity. This work resulted in the discovery of a potent c-Met inhibitor 23n, bearing 2-hydroxy-3-allylphenyl group at R(2) moiety, as a valuable lead molecule, which possessed remarkable cytotoxicity and high selectivity against A549 and HT-29 cell lines with IC50 values of 11nM and 27nM.
4.Discovery of 6-(difluoro(6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b][1,2,4]triazin-3-yl)methyl)quinoline as a highly potent and selective c-Met inhibitor.
Zhan Z1, Peng X2, Liu Q3, Chen F1, Ji Y2, Yao S1, Xi Y2, Lin Y1, Chen T3, Xu Y4, Ai J5, Geng M6, Duan W7. Eur J Med Chem. 2016 Mar 31;116:239-251. doi: 10.1016/j.ejmech.2016.03.076. [Epub ahead of print]
c-Met/HGF overexpression has been detected in many human malignancies including tumors which are resistant to anticancer therapy. Disrupting the aberrant c-Met/HGF axis has enjoyed significant progress in both preclinical and clinical antitumor campaign. To eliminate the OCH2-related metabolic deficiency of our previously reported triazolotriazine 2, we synthesized a series of CH2-/CF2-linked triazolotriazines and assessed their c-Met activities, leading to the highly potent compound 23 with IC50 values of 0.24 nM of enzymatic activity in c-Met and 0.85 nM of cellular activity in EBC-1 cancer cell line, as well as with complete tumor regression in EBC-1 xenograft mice model at dose of 25 mg/kg via oral administration. Based on its potent anti-proliferative activities and favorable pharmacokinetic properties, 23 has been selected as a drug candidate for preclinical investigation.
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CAS 1357072-61-7 c-Met inhibitor 1

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