Dovitinib-d8

Modify Date: 2024-01-18 17:04:34

Dovitinib-d8 Structure
Dovitinib-d8 structure
Common Name Dovitinib-d8
CAS Number 1246819-84-0 Molecular Weight 400.479
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C21H13D8FN6O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Dovitinib-d8


Dovitinib-D8 (CHIR-258-D8) is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively[1][2].

 Names

Name Dovitinib-d8
Synonym More Synonyms

 Dovitinib-d8 Biological Activity

Description Dovitinib-D8 (CHIR-258-D8) is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively[1][2].
Related Catalog
In Vitro Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
References

[1]. Cox L, et al. Levomepromazine for nausea and vomiting in palliative care. Cochrane Database Syst Rev. 2015;2015(11):CD009420. Published 2015 Nov 2.

[2]. Trudel S, et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 2005, 105(7), 2941-2948.

[3]. Huynh H, et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. J Hepatol. 2012, 56(3), 595-601.

[4]. Lee Y, et al. A Receptor Tyrosine Kinase Inhibitor, Dovitinib (TKI-258), Enhances BMP-2-Induced Osteoblast Differentiation In Vitro. Mol Cells. 2016 May 31;39(5):389-94

[5]. Chon HJ, et al. Traf2- and Nck-interacting kinase (TNIK) is involved in the anti-cancer mechanism of dovitinib in human multiple myeloma IM-9 cells. Amino Acids. 2016 Jul;48(7):1591-9.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Molecular Formula C21H13D8FN6O
Molecular Weight 400.479
Exact Mass 400.226288
LogP 1.59
Index of Refraction 1.691

 Synonyms

2(1H)-Quinolinone, 4-amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl-2,2,3,3,5,5,6,6-d8)-1H-benzimidazol-2-yl]-
Dovitinib-d8
4-Amino-5-fluoro-3-{6-[4-methyl(2H8)-1-piperazinyl]-1H-benzimidazol-2-yl}-2(1H)-quinolinone