N-Desethyl Sunitinib-d5

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N-Desethyl Sunitinib-d5 

N-Desethyl Sunitinib-d5 是 N-Desethyl Sunitinib 的氘代物。N-Desethyl Sunitinib (SU-12662) 是 Sunitinib 的代谢物。Sunitinib是有效的，ATP 竞争的 VEGFR，PDGFRβ 和 KIT 抑制剂，能够抑制 VEGFR -1，VEGFR -2，VEGFR -3，PDGFRβ 和 KIT 的活性，Ki 值分别为 2，9，17，8 和 4 nM。

N-Desethyl Sunitinib-d5

N-Desethyl Sunitinib-d5 Chemical Structure

CAS No. : 1217247-62-5

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生物活性

N-Desethyl Sunitinib-d5 is the deuterium labeled N-Desethyl Sunitinib. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively[1].

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

375.45

Formula

C20H18D5FN4O2
CAS 号

1217247-62-5
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Sun L, et al. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor r

    [3]. Mendel DB, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Can

    [4]. O’Farrell AM, et al. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood. 2003 May 1;101(9):3597-605. Epub 2003 Jan 16.

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