Dovitinib-D8(Synonyms: 多韦替尼 D8)

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Dovitinib-D8 (Synonyms: 多韦替尼 D8)

Dovitinib-D8 (CHIR-258-D8) 是 Dovitinib 的氘代物。Dovitinib (CHIR-258) 是多靶点的酪氨酸激酶抑制剂，抑制 FLT3，c-Kit，FGFR1/FGFR3，VEGFR1/VEGFR2/VEGFR3 和 PDGFRα/PDGFRβ 的 IC50 值分别为 1，2，8/9，10/13/8，27/210 nM。

Dovitinib-D8(Synonyms: 多韦替尼 D8)

Dovitinib-D8 Chemical Structure

CAS No. : 1246819-84-0

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生物活性

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].

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

400.48

Formula

C21H13D8FN6O
CAS 号

1246819-84-0
中文名称

多韦替尼 D8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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