Fostamatinib-d9(Synonyms: R788-d9)

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Fostamatinib-d9 (Synonyms: R788-d9)

Fostamatinib-d9 (R788-d9) 是 Fostamatinib 的氘代物。Fostamatinib (R788) 是 R406 的口服前药。R406 是一种有效的，具有口服活性的，ATP 竞争性的 Syk/FLT3 抑制剂，Ki 为 30 nM，IC50 为 41 nM。R406 还抑制 Lyn (IC50=63 nM) 和

Fostamatinib-d9(Synonyms: R788-d9)

Fostamatinib-d9 Chemical Structure

CAS No. : 1260832-60-7

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生物活性

Fostamatinib-d9 (R788-d9) is the deuterium labeled Fostamatinib. Fostamatinib (R788) is the oral prodrug of the active compound R406[1]. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM[2]. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[3].

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

589.51

Formula

C23H17D9FN6O9P
CAS 号

1260832-60-7
中文名称

福他替尼 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]. Stephen P McAdoo, et al. Fostamatinib Disodium. Drugs Future. 2011;36(4):273.

    [3]. Sylvia Braselmann, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008.

    [4]. Hoon-Suk Cha , et al. A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. J Pharmacol Exp Ther. 2006 May;317(2):571-8.

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