For research use only. Not for therapeutic Use.
Tivozanib（Cat No.:I003652）is a potent tyrosine kinase inhibitor that selectively targets vascular endothelial growth factor receptors (VEGFR-1, -2, and -3), playing a crucial role in inhibiting tumor angiogenesis. It is primarily used in the treatment of advanced renal cell carcinoma (RCC), where its high selectivity and prolonged activity offer improved efficacy with fewer off-target effects. Tivozanib’s ability to hinder blood vessel formation essential for tumor growth makes it a valuable therapeutic option in cancer therapy, especially in cases resistant to other treatments.
| Catalog Number | I003652 |
| CAS Number | 475108-18-0 |
| Synonyms | 1-[2-chloro-4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(5-methyl-1,2-oxazol-3-yl)urea |
| Molecular Formula | C₂₂H₁₉ClN₄O₅ |
| Purity | 98% |
| Target | VEGFR |
| Target Protein | |
| Solubility | DMSO ≥36mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
| Appearance | Solid |
| Storage | Dry, dark and at 2 - 8 °C for six months or -20°C for two years. |
| IC50 | VEGFR1：0.21 nM (IC50) |
| IUPAC Name | 1-[2-chloro-4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(5-methyl-1,2-oxazol-3-yl)urea |
| InChI | InChI=1S/C22H19ClN4O5/c1-12-8-21(27-32-12)26-22(28)25-16-5-4-13(9-15(16)23)31-18-6-7-24-17-11-20(30-3)19(29-2)10-14(17)18/h4-11H,1-3H3,(H2,25,26,27,28) |
| InChIKey | SPMVMDHWKHCIDT-UHFFFAOYSA-N |
| SMILES | CC1=CC(=NO1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)Cl |
| Reference | </br>1:Anti-tumour activity of tivozanib, a pan-inhibitor of VEGF receptors, in therapy-resistant ovarian carcinoma cells. Momeny M, Sabourinejad Z, Zarrinrad G, Moghaddaskho F, Eyvani H, Yousefi H, Mirshahvaladi S, Poursani EM, Barghi F, Poursheikhani A, Dardaei L, Bashash D, Ghazi-Khansari M, Tavangar SM, Dehpour AR, Yaghmaie M, Alimoghaddam K, Ghavamzadeh A, Ghaffari SH.Sci Rep. 2017 Apr 6;7:45954. doi: 10.1038/srep45954. PMID: 28383032 Free PMC Article</br>2:Blockade of vascular endothelial growth factor receptors by tivozanib has potential anti-tumour effects on human glioblastoma cells. Momeny M, Moghaddaskho F, Gortany NK, Yousefi H, Sabourinejad Z, Zarrinrad G, Mirshahvaladi S, Eyvani H, Barghi F, Ahmadinia L, Ghazi-Khansari M, Dehpour AR, Amanpour S, Tavangar SM, Dardaei L, Emami AH, Alimoghaddam K, Ghavamzadeh A, Ghaffari SH.Sci Rep. 2017 Mar 13;7:44075. doi: 10.1038/srep44075. PMID: 28287096 Free PMC Article</br>3:Targeting angiogenesis in advanced soft tissue sarcoma: tivozanib-hype or me-too? Mir O, Penel N.Ann Oncol. 2017 Jan 1;28(1):13-15. doi: 10.1093/annonc/mdw631. No abstract available. PMID: 28177430 </br>4:Targeting angiogenesis in advanced soft tissue sarcoma: Tivozanib – hype or me-too? Mir O, Penel N.Ann Oncol. 2016 Dec 19. pii: mdw631. doi: 10.1093/annonc/mdw631. [Epub ahead of print] No abstract available. PMID: 27998962 </br>5:Phase II study of tivozanib, an oral VEGFR inhibitor, in patients with recurrent glioblastoma. Kalpathy-Cramer J, Chandra V, Da X, Ou Y, Emblem KE, Muzikansky A, Cai X, Douw L, Evans JG, Dietrich J, Chi AS, Wen PY, Stufflebeam S, Rosen B, Duda DG, Jain RK, Batchelor TT, Gerstner ER.J Neurooncol. 2017 Feb;131(3):603-610. doi: 10.1007/s11060-016-2332-5. Epub 2016 Nov 16. PMID: 27853960 </br>6:A phase II study of tivozanib in patients with metastatic and nonresectable soft-tissue sarcomas. Agulnik M, Costa RLB, Milhem M, Rademaker AW, Prunder BC, Daniels D, Rhodes BT, Humphreys C, Abbinanti S, Nye L, Cehic R, Polish A, Vintilescu C, McFarland T, Skubitz K, Robinson S, Okuno S, Van Tine BA.Ann Oncol. 2017 Jan 1;28(1):121-127. doi: 10.1093/annonc/mdw444. PMID: 27771610 </br>7:BATON-CRC: A Phase II Randomized Trial Comparing Tivozanib Plus mFOLFOX6 with Bevacizumab Plus mFOLFOX6 in Stage IV Metastatic Colorectal Cancer. Benson AB 3rd, Kiss I, Bridgewater J, Eskens FA, Sasse C, Vossen S, Chen J, Van Sant C, Ball HA, Keating A, Krivoshik A.Clin Cancer Res. 2016 Oct 15;22(20):5058-5067. Epub 2016 Jul 11. PMID: 27401244 </br>8:Effects of ketoconazole or rifampin on the pharmacokinetics of tivozanib hydrochloride, a vascular endothelial growth factor receptor tyrosine kinase inhibitor. Cotreau MM, Siebers NM, Miller J, Strahs AL, Slichenmyer W.Clin Pharmacol Drug Dev. 2015 Mar;4(2):137-42. doi: 10.1002/cpdd.145. Epub 2014 Oct 1. PMID: 27128217 </br>9:Design, synthesis and biological evaluation of deuterated Tivozanib for improving pharmacokinetic properties. Guo S, Pang X, Peng L, Zhan M, Fan L, Gong Y, Kang F, Chen Y.Bioorg Med Chem Lett. 2015 Jun 1;25(11):2425-8. doi: 10.1016/j.bmcl.2015.03.088. Epub 2015 Apr 4. PMID: 25908516 </br>10:Tivozanib: status of development. Jamil MO, Hathaway A, Mehta A.Curr Oncol Rep. 2015 Jun;17(6):24. doi: 10.1007/s11912-015-0451-3. Review. PMID: 25895472 |
