Dovitinib

• CAT Number: I003476
• CAS Number: 405169-16-6
• Molecular Formula: C₂₁H₂₁FN₆O
• Molecular Weight: 392.43
• Purity: ≥95%
• Target: FGFR
• Solubility: DMSO: ≤ 25 mg/mL
• Storage: 3 years -20℃ powder
• IUPAC Name: 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one
• InChI: 1S/C21H21FN6O/c1-27-7-9-28(10-8-27)12-5-6-14-16(11-12)25-20(24-14)18-19(23)17-13(22)3-2-4-15(17)26-21(18)29/h2-6,11,24-25H,7-10,23H2,1H3/b20-18-
• InChIKey: KCOYQXZDFIIGCY-ZZEZOPTASA-N
• SMILES: CN1CCN(CC1)C2=CC3=C(C=C2)NC(=C4C(=C5C(=NC4=O)C=CC=C5F)N)N3

Dovitinib (Cat.No:I003476) is a small molecule multi-kinase inhibitor that targets various receptor tyrosine kinases involved in tumor growth and angiogenesis. It is being investigated for its potential in the treatment of solid tumors, including renal cell carcinoma and hepatocellular carcinoma. 

Reference

1:Dovitinib enhances temozolomide efficacy in glioblastoma cells. Thanasupawat T, Natarajan S, Rommel A, Glogowska A, Bergen H, Krcek J, Pitz M, Beiko J, Krawitz S, Verma IM, Ghavami S, Klonisch T, Hombach-Klonisch S.Mol Oncol. 2017 May 13. doi: 10.1002/1878-0261.12076. [Epub ahead of print] PMID: 28500786 Free Article2:Synergistic inhibition effect of TNIK inhibitor KY-05009 and receptor tyrosine kinase inhibitor dovitinib on IL-6-induced proliferation and Wnt signaling pathway in human multiple myeloma cells. Lee Y, Jung JI, Park KY, Kim SA, Kim J.Oncotarget. 2017 Apr 12. doi: 10.18632/oncotarget.17056. [Epub ahead of print] PMID: 28467797 Free Article3:Co-clinical trials demonstrate predictive biomarkers for dovitinib, an FGFR inhibitor, in lung squamous cell carcinoma. Kim HR, Kang HN, Shim HS, Kim EY, Kim J, Kim DJ, Lee JG, Lee CY, Hong MH, Kim SM, Kim H, Pyo KH, Yun MR, Park HJ, Han JY, Youn HA, Ahn MJ, Paik S, Kim TM, Cho BC.Ann Oncol. 2017 Apr 27. doi: 10.1093/annonc/mdx098. [Epub ahead of print] PMID: 28460066 4:A Phase II study of Dovitinib in Patients With Recurrent or Metastatic Adenoid Cystic Carcinoma. Dillon PM, Petroni GR, Horton BJ, Moskaluk CA, Fracasso PM, Douvas MG, Varhegyi N, Zaja-Milatovic S, Thomas CY.Clin Cancer Res. 2017 Apr 4. pii: clincanres.2942.2016. doi: 10.1158/1078-0432.CCR-16-2942. [Epub ahead of print] PMID: 28377480 5:Induction of Neuroendocrine Differentiation in Prostate Cancer Cells by Dovitinib (TKI-258) and its Therapeutic Implications. Yadav SS, Li J, Stockert JA, Herzog B, O/’Connor J, Garzon-Manco L, Parsons R, Tewari AK, Yadav KK.Transl Oncol. 2017 Jun;10(3):357-366. doi: 10.1016/j.tranon.2017.01.011. Epub 2017 Mar 24. PMID: 28342996 Free PMC Article6:A phase II trial of dovitinib in previously-treated advanced pleural mesothelioma: The Ontario Clinical Oncology Group. Laurie SA, Hao D, Leighl NB, Goffin J, Khomani A, Gupta A, Addison CL, Bane A, Seely J, Filion ML, Pond GR, Levine MN.Lung Cancer. 2017 Feb;104:65-69. doi: 10.1016/j.lungcan.2016.12.004. Epub 2016 Dec 15. PMID: 28213002 7:Phase II, randomized, placebo-controlled study of dovitinib in combination with fulvestrant in postmenopausal patients with HR+, HER2- breast cancer that had progressed during or after prior endocrine therapy. Musolino A, Campone M, Neven P, Denduluri N, Barrios CH, Cortes J, Blackwell K, Soliman H, Kahan Z, Bonnefoi H, Squires M, Zhang Y, Deudon S, Shi MM, André F.Breast Cancer Res. 2017 Feb 10;19(1):18. doi: 10.1186/s13058-017-0807-8. PMID: 28183331 Free PMC Article8:A Phase II Trial of Dovitinib in BCG-Unresponsive Urothelial Carcinoma with FGFR3 Mutations or Overexpression: Hoosier Cancer Research Network Trial HCRN 12-157. Hahn NM, Bivalacqua TJ, Ross AE, Netto GJ, Baras A, Park JC, Chapman C, Masterson TA, Koch MO, Bihrle R, Foster RS, Gardner TA, Cheng L, Jones DR, McElyea K, Sandusky GE, Breen T, Liu Z, Albany C, Moore ML, Loman RL, Reed A, Turner SA, De Abreu FB, Gallagher T, Tsongalis GJ, Plimack ER, Greenberg RE, Geynisman DM.Clin Cancer Res. 2016 Dec 8. doi: 10.1158/1078-0432.CCR-16-2267. [Epub ahead of print] PMID: 27932416 9:Randomized phase 1 crossover study assessing the bioequivalence of capsule and tablet formulations of dovitinib (TKI258) in patients with advanced solid tumors. Sarantopoulos J, Goel S, Chung V, Munster P, Pant S, Patel MR, Infante J, Tawbi H, Becerra C, Bruce J, Kabbinavar F, Lockhart AC, Tan E, Yang S, Carlson G, Scott JW, Sharma S.Cancer Chemother Pharmacol. 2016 Nov;78(5):921-927. Epub 2016 Sep 28. PMID: 27681579 10:Efficacy and safety of dovitinib in pretreated patients with advanced squamous non-small cell lung cancer with FGFR1 amplification: A single-arm, phase 2 study. Lim SH, Sun JM, Choi YL, Kim HR, Ahn S, Lee JY, Lee SH, Ahn JS, Park K, Kim JH, Cho BC, Ahn MJ.Cancer. 2016 Oct;122(19):3024-31. doi: 10.1002/cncr.30135. Epub 2016 Jun 17. PMID: 27315356