1246819-84-0

1246819-84-0 structure

Name: Dovitinib-d8
Chemical Name: Dovitinib-d8
CAS Number: 1246819-84-0
Molecular Formula: C₂₁H₁₃D₈FN₆O
Molecular Weight: 400.479
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK c-Kit
Create Date: 2021-05-04 11:49:49
Modify Date: 2024-01-18 17:04:34
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].

Name	Dovitinib-d8
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

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	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3 Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit
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.

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

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