Brigatinib-13C6(Synonyms: AP-26113-13C6)

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Brigatinib-13C6 (Synonyms: AP-26113-13C6)

Brigatinib-13C6 (AP-26113-13C6) 是一种 13C 标记的 Brigatinib。Brigatinib (AP-26113) 是有效,选择性的 ALK 抑制剂,IC50 值为 0.6 nM。

Brigatinib-13C6(Synonyms: AP-26113-13C6)

Brigatinib-13C6 Chemical Structure

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生物活性

Brigatinib-13C6 (AP-26113-13C6) is the 13C-labeled Brigatinib. Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor, with an IC50 of 0.6 nM[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

590.05

Formula

C2313C6H39ClN7O2P

中文名称

布格替尼 13C6

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]. Zhang S, et al. The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models. Clin Cancer Res. 2016 Nov 15;22(22):5527-5538

    [3]. Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016 May 26;59(10):4948-64.

    [4]. Siaw JT, et al. Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice. Oncotarget. 2016 May 17;7(20):29011-22

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