Dovitinib lactate
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 200760

CAS#: 915769-50-5 (lactate)

Description: Dovitinib, also known as TKI-258 or CHIR-258, is an orally bioavailable FGFR3 inhibitor, which strongly binds to fibroblast growth factor receptor 3 (FGFR3) and inhibits its phosphorylation, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell death. In addition, this agent may inhibit other members of the RTK superfamily, including the vascular endothelial growth factor receptor; fibroblast growth factor receptor 1; platelet-derived growth factor receptor type 3; FMS-like tyrosine kinase 3; stem cell factor receptor (c-KIT); and colony-stimulating factor receptor 1; this may result in an additional reduction in cellular proliferation and angiogenesis, and the induction of tumor cell apoptosis.


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 650
1g
USD 2650
Size
Price

25mg
USD 250
200mg
USD 950
2g
USD 4250
Size
Price

50mg
USD 450
500mg
USD 1450
5g
USD 7850

Dovitinib lactate, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 200760
Name: Dovitinib lactate
CAS#: 915769-50-5 (lactate)
Chemical Formula: C24H27FN6O4
Exact Mass:
Molecular Weight: 482.51
Elemental Analysis: C, 59.74; H, 5.64; F, 3.94; N, 17.42; O, 13.26


Related CAS #: 915769-50-5 (lactate)   405169-16-6 (free base)    

Synonym: TKI258; TKI-258; TKI 258; CHIR258; CHIR-258; CHIR 258; Dovitinib lactate

IUPAC/Chemical Name: 4-Amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-2(1H)-quinolinone 2-hydroxypropanoate

InChi Key: ZRHDKBOBHHFLBW-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H21FN6O.C3H6O3/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;1-2(4)3(5)6/h2-6,11H,7-10H2,1H3,(H,24,25)(H3,23,26,29);2,4H,1H3,(H,5,6)

SMILES Code: O=C1NC2=C(C(F)=CC=C2)C(N)=C1C3=NC4=CC=C(N5CCN(C)CC5)C=C4N3.CC(O)C(O)=O


Technical Data

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

 
 


References

1: Pilié P, Hasanov E, Matin SF, Woodson AHH, Marcott VD, Bird S, Slack RS, Fuller GN, McCutcheon IE, Jonasch E. Pilot study of dovitinib in patients with von Hippel-Lindau disease. Oncotarget. 2018 May 4;9(34):23390-23395. doi: 10.18632/oncotarget.25171. eCollection 2018 May 4. PubMed PMID: 29805741; PubMed Central PMCID: PMC5955100.

2: Choi YJ, Kim HS, Park SH, Kim BS, Kim KH, Lee HJ, Song HS, Shin DY, Lee HY, Kim HG, Lee KH, Lee JL, Park KH. Phase II Study of Dovitinib in Patients with Castration-Resistant Prostate Cancer (KCSG-GU11-05). Cancer Res Treat. 2018 Jan 2. doi: 10.4143/crt.2017.438. [Epub ahead of print] PubMed PMID: 29334610.

3: de Weger VA, Goel S, von Moos R, Schellens JHM, Mach N, Tan E, Anand S, Scott JW, Lassen U. A drug-drug interaction study to assess the effect of the CYP1A2 inhibitor fluvoxamine on the pharmacokinetics of dovitinib (TKI258) in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2018 Jan;81(1):73-80. doi: 10.1007/s00280-017-3469-4. Epub 2017 Nov 3. PubMed PMID: 29101463.

4: Shivapurkar N, Vietsch EE, Carney E, Isaacs C, Wellstein A. Circulating microRNAs in patients with hormone receptor-positive, metastatic breast cancer treated with dovitinib. Clin Transl Med. 2017 Oct 4;6(1):37. doi: 10.1186/s40169-017-0169-y. PubMed PMID: 28980224; PubMed Central PMCID: PMC5628092.

5: Landberg N, Dreimane A, Rissler M, Billström R, Ågerstam H. Primary cells in BCR/FGFR1-positive 8p11 myeloproliferative syndrome are sensitive to dovitinib, ponatinib, and dasatinib. Eur J Haematol. 2017 Nov;99(5):442-448. doi: 10.1111/ejh.12957. Epub 2017 Oct 4. PubMed PMID: 28881484.

6: Joensuu H, Blay JY, Comandone A, Martin-Broto J, Fumagalli E, Grignani G, Del Muro XG, Adenis A, Valverde C, Pousa AL, Bouché O, Italiano A, Bauer S, Barone C, Weiss C, Crippa S, Camozzi M, Castellana R, Le Cesne A. Dovitinib in patients with gastrointestinal stromal tumour refractory and/or intolerant to imatinib. Br J Cancer. 2017 Oct 24;117(9):1278-1285. doi: 10.1038/bjc.2017.290. Epub 2017 Aug 29. PubMed PMID: 28850565; PubMed Central PMCID: PMC5672922.

7: Semrad TJ, Kim EJ, Tanaka MS, Sands J, Roberts C, Burich RA, Li Y, Gandara DR, Lara P Jr, Mack PC. Phase II Study of Dovitinib in Patients Progressing on Anti-Vascular Endothelial Growth Factor Therapy. Cancer Treat Res Commun. 2017;10:21-26. doi: 10.1016/j.ctarc.2016.12.002. PubMed PMID: 28736761; PubMed Central PMCID: PMC5519297.

8: Baek SW, Seo YJ, Lee HJ. Multiple milia associated with use of the tyrosine kinase inhibitor dovitinib. Australas J Dermatol. 2018 Feb;59(1):57-58. doi: 10.1111/ajd.12620. Epub 2017 Jun 21. PubMed PMID: 28636150.

9: 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. Dovitinib enhances temozolomide efficacy in glioblastoma cells. Mol Oncol. 2017 Aug;11(8):1078-1098. doi: 10.1002/1878-0261.12076. Epub 2017 Jun 5. PubMed PMID: 28500786; PubMed Central PMCID: PMC5537714.

10: Lee Y, Jung JI, Park KY, Kim SA, Kim J. 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. Oncotarget. 2017 Jun 20;8(25):41091-41101. doi: 10.18632/oncotarget.17056. PubMed PMID: 28467797; PubMed Central PMCID: PMC5522218.

11: 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. Co-clinical trials demonstrate predictive biomarkers for dovitinib, an FGFR inhibitor, in lung squamous cell carcinoma. Ann Oncol. 2017 Jun 1;28(6):1250-1259. doi: 10.1093/annonc/mdx098. PubMed PMID: 28460066.

12: Dillon PM, Petroni GR, Horton BJ, Moskaluk CA, Fracasso PM, Douvas MG, Varhegyi N, Zaja-Milatovic S, Thomas CY. A Phase II Study of Dovitinib in Patients with Recurrent or Metastatic Adenoid Cystic Carcinoma. Clin Cancer Res. 2017 Aug 1;23(15):4138-4145. doi: 10.1158/1078-0432.CCR-16-2942. Epub 2017 Apr 4. PubMed PMID: 28377480; PubMed Central PMCID: PMC5540767.

13: Yadav SS, Li J, Stockert JA, Herzog B, O'Connor J, Garzon-Manco L, Parsons R, Tewari AK, Yadav KK. Induction of Neuroendocrine Differentiation in Prostate Cancer Cells by Dovitinib (TKI-258) and its Therapeutic Implications. Transl Oncol. 2017 Jun;10(3):357-366. doi: 10.1016/j.tranon.2017.01.011. Epub 2017 Mar 24. PubMed PMID: 28342996; PubMed Central PMCID: PMC5369368.

14: Laurie SA, Hao D, Leighl NB, Goffin J, Khomani A, Gupta A, Addison CL, Bane A, Seely J, Filion ML, Pond GR, Levine MN. A phase II trial of dovitinib in previously-treated advanced pleural mesothelioma: The Ontario Clinical Oncology Group. Lung Cancer. 2017 Feb;104:65-69. doi: 10.1016/j.lungcan.2016.12.004. Epub 2016 Dec 15. PubMed PMID: 28213002.

15: 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. 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. Breast Cancer Res. 2017 Feb 10;19(1):18. doi: 10.1186/s13058-017-0807-8. PubMed PMID: 28183331; PubMed Central PMCID: PMC5301372.

16: 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. A Phase II Trial of Dovitinib in BCG-Unresponsive Urothelial Carcinoma with FGFR3 Mutations or Overexpression: Hoosier Cancer Research Network Trial HCRN 12-157. Clin Cancer Res. 2017 Jun 15;23(12):3003-3011. doi: 10.1158/1078-0432.CCR-16-2267. Epub 2016 Dec 8. PubMed PMID: 27932416; PubMed Central PMCID: PMC5462889.

17: 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. Randomized phase 1 crossover study assessing the bioequivalence of capsule and tablet formulations of dovitinib (TKI258) in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2016 Nov;78(5):921-927. Epub 2016 Sep 28. PubMed PMID: 27681579.

18: Lim SH, Sun JM, Choi YL, Kim HR, Ahn S, Lee JY, Lee SH, Ahn JS, Park K, Kim JH, Cho BC, Ahn MJ. 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. Cancer. 2016 Oct;122(19):3024-31. doi: 10.1002/cncr.30135. Epub 2016 Jun 17. PubMed PMID: 27315356.

19: Schäfer N, Gielen GH, Kebir S, Wieland A, Till A, Mack F, Schaub C, Tzaridis T, Reinartz R, Niessen M, Fimmers R, Simon M, Coch C, Fuhrmann C, Herrlinger U, Scheffler B, Glas M. Phase I trial of dovitinib (TKI258) in recurrent glioblastoma. J Cancer Res Clin Oncol. 2016 Jul;142(7):1581-9. doi: 10.1007/s00432-016-2161-0. Epub 2016 Apr 21. PubMed PMID: 27100354.

20: Cheng AL, Thongprasert S, Lim HY, Sukeepaisarnjaroen W, Yang TS, Wu CC, Chao Y, Chan SL, Kudo M, Ikeda M, Kang YK, Pan H, Numata K, Han G, Balsara B, Zhang Y, Rodriguez AM, Zhang Y, Wang Y, Poon RT. Randomized, open-label phase 2 study comparing frontline dovitinib versus sorafenib in patients with advanced hepatocellular carcinoma. Hepatology. 2016 Sep;64(3):774-84. doi: 10.1002/hep.28600. Epub 2016 May 17. PubMed PMID: 27082062.