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文件名称:Fedratinib-d9-TG-101348-d-sub-9-sub-生命科学试剂-MCE.pdf
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更新时间:2025-06-12
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文档摘要

Hotline:400-820-3792

Inhibitors?ScreeningLibraries?Proteins

www.MedChemE

Fedratinib-d9

Cat.No.:HY-10409S

Synonyms:TG-101348-d;SAR302503-d

99

分?式:C??H??D?N?O?S

分?量:533.73

作?靶点:Isotope-LabeledCompounds;Apoptosis;JAK

作?通路:Others;Apoptosis;Epigenetics;JAK/STATSignaling;Protein

TyrosineKinase/RTK;StemCell/Wnt

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性Fedratinib-d9(TG-101348-d9)是氘代标记的Fedratinib。Fedratinib(TG-101348)是?种有效的,选择性的

,ATP竞争性和具有?服活性的JAK2抑制剂,对于JAK2和JAK2V617F激酶的IC50均为3nM。Fedratinib

对JAK2的选择性分别?JAK1和JAK3?35倍和334倍。Fedratinib可诱导癌细胞凋亡(apoptosis),并可?

于?髓增?性疾病的研究。

REFERENCES

[1].RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019

Feb;53(2):211-216.

[2].GeronI,etal.SelectiveinhibitionofJAK2-drivenerythroiddifferentiationofpolycythemiaveraprogenitors.CancerCell.2008

Apr;13(4):321-30.

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