Nolatrexed-d4 dihydrochloride(Synonyms: 盐酸诺拉曲塞 d4 (双盐酸盐))

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Nolatrexed-d4 dihydrochloride (Synonyms: 盐酸诺拉曲塞 d4 (双盐酸盐))

Nolatrexed-d4 dihydrochloride 是 Nolatrexed dihydrochloride 的氘代物。Nolatrexed dihydrochloride (AG 337) 是一种非竞争性的胸苷酸合酶 (thymidylate synthase) 抑制剂，与该酶的叶酸辅因子结合位点相互作用，对人 thymidylate synthase 的 Ki 值为 11 nM。Nolatrexed dihydrochloride (AG 337) 能够在癌细胞 S 期诱导细胞周期停滞。具有抗癌活性。

Nolatrexed-d4 dihydrochloride(Synonyms: 盐酸诺拉曲塞 d4 (双盐酸盐))

Nolatrexed-d4 dihydrochloride Chemical Structure

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生物活性

Nolatrexed-d4 dihydrochloride (AG 337-d4) is the deuterium labeled Nolatrexed dihydrochloride. Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase[1]. Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity[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

361.28

Formula

C14H10D4Cl2N4OS
中文名称

盐酸诺拉曲塞 d4 (双盐酸盐)
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]. Webber S, et al. AG337, a novel lipophilic thymidylate synthase inhibitor: in vitro and in vivo preclinical studies. Cancer Chemother Pharmacol. 1996;37(6):509-17.

    [3]. McGuire JJ, et al. Characterization of the effect of AG337, a novel lipophilic thymidylate synthase inhibitor, on human head and neck and human leukemia cell lines.

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