Dabrafenib-d9(Synonyms: GSK2118436A-d9; GSK2118436-d9)

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Dabrafenib-d9 (Synonyms: GSK2118436A-d9; GSK2118436-d9)

Dabrafenib-d9 (GSK2118436A-d9) 是 Dabrafenib 的氘代物。Dabrafenib (GSK2118436A) 是ATP竞争型的 Raf 抑制剂,抑制 C-RafB-RafV600EIC50 分别为 5 nM 和 0.6 nM。

Dabrafenib-d9(Synonyms: GSK2118436A-d9;  GSK2118436-d9)

Dabrafenib-d9 Chemical Structure

CAS No. : 1423119-98-5

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生物活性

Dabrafenib-d9 (GSK2118436A-d9) is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively[4].

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

528.62

Formula

C23H11D9F3N5O2S2

CAS 号

1423119-98-5

中文名称

达拉非尼 d9

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]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther, 2012, 11(4), 909-920.

    [3]. Lee S, et al. Anti-inflammatory effects of dabrafenib on polyphosphate-mediated vascular disruption. Chem Biol Interact. 2016 Jul 22.

    [4]. Jung B, et al. Anti-septic effects of dabrafenib on HMGB1-mediated inflammatory responses. BMB Rep. 2016 Apr;49(4):214-9.

    [5]. Alexander M Menzies, et al. Dabrafenib and its potential for the treatment of metastatic melanoma. Drug Des Devel Ther. 2012; 6: 391–405.

    [6]. Posobiec LM, et al. Early Vaginal Opening in Juvenile Female Rats Given BRAF-Inhibitor Dabrafenib Is Not Associated with Early Physiologic Sexual Maturation. Birth Defects Res B Dev Reprod Toxicol. 2015 Dec;104(6):244-52.

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