For research use only. Not for therapeutic Use.
Tivantinib (Cat No.:I005412) is a small-molecule inhibitor of the MET receptor tyrosine kinase, which is involved in signaling pathways related to cell growth, survival, and metastasis. By selectively targeting and inhibiting the MET receptor, tivantinib interferes with MET-dependent cellular processes and inhibits tumor growth and metastasis. It has shown potential in the treatment of various cancers, including non-small cell lung cancer (NSCLC) and hepatocellular carcinoma (HCC). Tivantinib’s ability to inhibit MET signaling makes it an attractive candidate for targeted therapy, either as a monotherapy or in combination with other anticancer agents, providing a potential treatment option for patients with MET-positive tumors.
| Catalog Number | I005412 |
| CAS Number | 905854-02-6 |
| Synonyms | (3S,4R)-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione |
| Molecular Formula | C₂₃H₁₉N₃O₂ |
| Purity | ≥95% |
| Target | c-MET |
| Solubility | 10 mM in DMSO |
| Storage | 3 years -20C powder |
| IC50 | 0.355 μM(Ki) |
| IUPAC Name | (3R,4R)-3-(1-azatricyclo[6.3.1.04,12]dodeca-2,4,6,8(12)-tetraen-3-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione |
| InChI | InChI=1S/C23H19N3O2/c27-22-19(16-11-24-18-9-2-1-7-14(16)18)20(23(28)25-22)17-12-26-10-4-6-13-5-3-8-15(17)21(13)26/h1-3,5,7-9,11-12,19-20,24H,4,6,10H2,(H,25,27,28)/t19-,20-/m0/s1 |
| InChIKey | UCEQXRCJXIVODC-PMACEKPBSA-N |
| SMILES | C1CC2=C3C(=CC=C2)C(=CN3C1)[C@H]4[C@@H](C(=O)NC4=O)C5=CNC6=CC=CC=C65 |
| Reference | </br>1:A phase 1 study of the c-Met inhibitor, tivantinib (ARQ197) in children with relapsed or refractory solid tumors: A Children/’s Oncology Group study phase 1 and pilot consortium trial (ADVL1111). Geller JI, Perentesis JP, Liu X, Minard CG, Kudgus RA, Reid JM, Fox E, Blaney SM, Weigel BJ.Pediatr Blood Cancer. 2017 Apr 27. doi: 10.1002/pbc.26565. [Epub ahead of print] PMID: 28449393 </br>2:Tivantinib for the treatment of hepatocellular carcinoma. Best J, Schotten C, Lohmann G, Gerken G, Dechêne A.Expert Opin Pharmacother. 2017 May;18(7):727-733. doi: 10.1080/14656566.2017.1316376. Epub 2017 Apr 17. PMID: 28414564 </br>3:Phase II study of the c-MET inhibitor tivantinib (ARQ 197) in patients with relapsed or relapsed/refractory multiple myeloma. Baljevic M, Zaman S, Baladandayuthapani V, Lin YH, de Partovi CM, Berkova Z, Amini B, Thomas SK, Shah JJ, Weber DM, Fu M, Cleeland CS, Wang XS, Stellrecht CM, Davis RE, Gandhi V, Orlowski RZ.Ann Hematol. 2017 Jun;96(6):977-985. doi: 10.1007/s00277-017-2980-3. Epub 2017 Mar 23. PMID: 28337527 Free PMC Article</br>4:Proliferation markers are associated with MET expression in hepatocellular carcinoma and predict tivantinib sensitivity in vitro. Rebouissou S, La Bella T, Rekik S, Imbeaud S, Calatayud AL, Rorh-Udilova N, Martin Y, Couchy G, Bioulac-Sage P, Grasl-Kraupp B, de Koning L, Ganne-Carrie N, Nault JC, Ziol M, Zucman-Rossi J.Clin Cancer Res. 2017 Feb 28. pii: clincanres.3118.2016. doi: 10.1158/1078-0432.CCR-16-3118. [Epub ahead of print] PMID: 28246274 </br>5:A phase I study of tivantinib in combination with temsirolimus in patients with advanced solid tumors. Kyriakopoulos CE, Braden AM, Kolesar JM, Eickhoff JC, Bailey HH, Heideman J, Liu G, Wisinski KB.Invest New Drugs. 2017 Jun;35(3):290-297. doi: 10.1007/s10637-016-0418-8. Epub 2016 Dec 21. PMID: 28004284 </br>6:Profile of tivantinib and its potential in the treatment of hepatocellular carcinoma: the evidence to date. Pievsky D, Pyrsopoulos N.J Hepatocell Carcinoma. 2016 Nov 15;3:69-76. eCollection 2016. Review. PMID: 27896243 Free PMC Article</br>7:Phase II study of erlotinib plus tivantinib (ARQ 197) in patients with locally advanced or metastatic EGFR mutation-positive non-small-cell lung cancer just after progression on EGFR-TKI, gefitinib or erlotinib. Azuma K, Hirashima T, Yamamoto N, Okamoto I, Takahashi T, Nishio M, Hirata T, Kubota K, Kasahara K, Hida T, Yoshioka H, Nakanishi K, Akinaga S, Nishio K, Mitsudomi T, Nakagawa K.ESMO Open. 2016 Jul 21;1(4):e000063. eCollection 2016. PMID: 27843623 Free PMC Article</br>8:Tumor and circulating biomarkers in patients with second-line hepatocellular carcinoma from the randomized phase II study with tivantinib. Rimassa L, Abbadessa G, Personeni N, Porta C, Borbath I, Daniele B, Salvagni S, Van Laethem JL, Van Vlierberghe H, Trojan J, De Toni EN, Weiss A, Miles S, Gasbarrini A, Lencioni M, Lamar ME, Wang Y, Shuster D, Schwartz BE, Santoro A.Oncotarget. 2016 Nov 8;7(45):72622-72633. doi: 10.18632/oncotarget.11621. PMID: 27579536 Free PMC Article</br>9:Quantitative analysis of tivantinib in rat plasma using ultra performance liquid chromatography with tandem mass spectrometry. Bai YL, Yuan HC, Zhang DT, Liu Y, Zhang Y.J Pharm Biomed Anal. 2016 Jul 15;126:98-102. doi: 10.1016/j.jpba.2016.05.003. Epub 2016 May 2. PMID: 27179187 </br>10:Allosteric inhibition of c-Met kinase in sub-microsecond molecular dynamics simulations induced by its inhibitor, tivantinib. Yan M, Wang H, Wang Q, Zhang Z, Zhang C.Phys Chem Chem Phys. 2016 Apr 21;18(15):10367-74. doi: 10.1039/c5cp07001e. Epub 2016 Mar 31. PMID: 27029952 |
