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Cytotoxic activity of tivantinib (ARQ 197) is not due solely to c-MET inhibition.

Katayama R, Aoyama A, Yamori T, Qi J, Oh-hara T, Song Y, Engelman JA, Fujita N.

Cancer Res. 2013 May 15;73(10):3087-96. doi: 10.1158/0008-5472.CAN-12-3256. Epub 2013 Apr 18.


Tivantinib (ARQ197) displays cytotoxic activity that is independent of its ability to bind MET.

Basilico C, Pennacchietti S, Vigna E, Chiriaco C, Arena S, Bardelli A, Valdembri D, Serini G, Michieli P.

Clin Cancer Res. 2013 May 1;19(9):2381-92. doi: 10.1158/1078-0432.CCR-12-3459. Epub 2013 Mar 26.


Tivantinib induces G2/M arrest and apoptosis by disrupting tubulin polymerization in hepatocellular carcinoma.

Xiang Q, Zhen Z, Deng DY, Wang J, Chen Y, Li J, Zhang Y, Wang F, Chen N, Chen H, Chen Y.

J Exp Clin Cancer Res. 2015 Oct 12;34:118. doi: 10.1186/s13046-015-0238-2.


Tivantinib (ARQ 197) efficacy is independent of MET inhibition in non-small-cell lung cancer cell lines.

Calles A, Kwiatkowski N, Cammarata BK, Ercan D, Gray NS, Jänne PA.

Mol Oncol. 2015 Jan;9(1):260-9. doi: 10.1016/j.molonc.2014.08.011. Epub 2014 Aug 29.


Tivantinib (ARQ 197) exhibits antitumor activity by directly interacting with tubulin and overcomes ABC transporter-mediated drug resistance.

Aoyama A, Katayama R, Oh-Hara T, Sato S, Okuno Y, Fujita N.

Mol Cancer Ther. 2014 Dec;13(12):2978-90. doi: 10.1158/1535-7163.MCT-14-0462. Epub 2014 Oct 13.


Targeting the pro-survival protein MET with tivantinib (ARQ 197) inhibits growth of multiple myeloma cells.

Zaman S, Shentu S, Yang J, He J, Orlowski RZ, Stellrecht CM, Gandhi V.

Neoplasia. 2015 Mar;17(3):289-300. doi: 10.1016/j.neo.2015.01.006.


Cabozantinib and Tivantinib, but Not INC280, Induce Antiproliferative and Antimigratory Effects in Human Neuroendocrine Tumor Cells in vitro: Evidence for 'Off-Target' Effects Not Mediated by c-Met Inhibition.

Reuther C, Heinzle V, Spampatti M, Vlotides G, de Toni E, Spöttl G, Maurer J, Nölting S, Göke B, Auernhammer CJ.

Neuroendocrinology. 2016;103(3-4):383-401. doi: 10.1159/000439431. Epub 2015 Aug 25.


Tivantinib (ARQ-197) exhibits anti-tumor activity with down-regulation of FAK in oral squamous cell carcinoma.

Xi WH, Yang LY, Cao ZY, Qian Y.

Biochem Biophys Res Commun. 2015 Feb 20;457(4):723-9. doi: 10.1016/j.bbrc.2015.01.062. Epub 2015 Jan 24.


Tivantinib (ARQ 197) affects the apoptotic and proliferative machinery downstream of c-MET: role of Mcl-1, Bcl-xl and Cyclin B1.

Lu S, Török HP, Gallmeier E, Kolligs FT, Rizzani A, Arena S, Göke B, Gerbes AL, De Toni EN.

Oncotarget. 2015 Sep 8;6(26):22167-78.


Targeted therapies: Tivantinib--a cytotoxic drug in MET inhibitor's clothes?

Michieli P, Di Nicolantonio F.

Nat Rev Clin Oncol. 2013 Jul;10(7):372-4. doi: 10.1038/nrclinonc.2013.86. Epub 2013 May 28. No abstract available.


Breast cancer-derived bone metastasis can be effectively reduced through specific c-MET inhibitor tivantinib (ARQ 197) and shRNA c-MET knockdown.

Previdi S, Abbadessa G, Dalò F, France DS, Broggini M.

Mol Cancer Ther. 2012 Jan;11(1):214-23. doi: 10.1158/1535-7163.MCT-11-0277. Epub 2011 Oct 25.


Tivantinib: critical review with a focus on hepatocellular carcinoma.

Rota Caremoli E, Labianca R.

Expert Opin Investig Drugs. 2014 Nov;23(11):1563-74. doi: 10.1517/13543784.2014.949339. Review.


Off-target effects of c-MET inhibitors on thyroid cancer cells.

Zhou Y, Zhao C, Gery S, Braunstein GD, Okamoto R, Alvarez R, Miles SA, Doan NB, Said JW, Gu J, Phillip Koeffler H.

Mol Cancer Ther. 2014 Jan;13(1):134-43. doi: 10.1158/1535-7163.MCT-13-0187. Epub 2013 Oct 29.


Synergistic activity of the c-Met and tubulin inhibitor tivantinib (ARQ197) with pemetrexed in mesothelioma cells.

Leon LG, Gemelli M, Sciarrillo R, Avan A, Funel N, Giovannetti E.

Curr Drug Targets. 2014;15(14):1331-40.


Tivantinib (ARQ197) displays cytotoxic activity that is independent of its ability to bind MET--letter.

Rimassa L, Bruix J, Broggini M, Santoro A.

Clin Cancer Res. 2013 Aug 1;19(15):4290. doi: 10.1158/1078-0432.CCR-13-1321. Epub 2013 Jun 13. No abstract available.


Tivantinib (ARQ197) displays cytotoxic activity that is independent of its ability to bind MET--response.

Michieli P, Basilico C, Pennacchietti S.

Clin Cancer Res. 2013 Aug 1;19(15):4291. doi: 10.1158/1078-0432.CCR-13-1534. Epub 2013 Jun 13. No abstract available.


ARQ 197, a novel and selective inhibitor of the human c-Met receptor tyrosine kinase with antitumor activity.

Munshi N, Jeay S, Li Y, Chen CR, France DS, Ashwell MA, Hill J, Moussa MM, Leggett DS, Li CJ.

Mol Cancer Ther. 2010 Jun;9(6):1544-53. doi: 10.1158/1535-7163.MCT-09-1173. Epub 2010 May 18.


A randomized, double-blind, placebo-controlled, phase III trial of erlotinib with or without a c-Met inhibitor tivantinib (ARQ 197) in Asian patients with previously treated stage IIIB/IV nonsquamous nonsmall-cell lung cancer harboring wild-type epidermal growth factor receptor (ATTENTION study).

Yoshioka H, Azuma K, Yamamoto N, Takahashi T, Nishio M, Katakami N, Ahn MJ, Hirashima T, Maemondo M, Kim SW, Kurosaki M, Akinaga S, Park K, Tsai CM, Tamura T, Mitsudomi T, Nakagawa K.

Ann Oncol. 2015 Oct;26(10):2066-72. doi: 10.1093/annonc/mdv288. Epub 2015 Jul 7.


Antitumor action of the MET tyrosine kinase inhibitor crizotinib (PF-02341066) in gastric cancer positive for MET amplification.

Okamoto W, Okamoto I, Arao T, Kuwata K, Hatashita E, Yamaguchi H, Sakai K, Yanagihara K, Nishio K, Nakagawa K.

Mol Cancer Ther. 2012 Jul;11(7):1557-64. doi: 10.1158/1535-7163.MCT-11-0934. Epub 2012 Jun 22.


Phase 1 dose-escalation trial evaluating the combination of the selective MET (mesenchymal-epithelial transition factor) inhibitor tivantinib (ARQ 197) plus erlotinib.

Goldman JW, Laux I, Chai F, Savage RE, Ferrari D, Garmey EG, Just RG, Rosen LS.

Cancer. 2012 Dec 1;118(23):5903-11. doi: 10.1002/cncr.27575. Epub 2012 May 17.

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