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文件名称:Crizotinib-d9-PF-02341066-d-sub-9-sub-生命科学试剂-MCE.pdf
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文档摘要

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Inhibitors?ScreeningLibraries?Proteins

www.MedChemE

Crizotinib-d9

Cat.No.:HY-50878S2

CASNo.:1523580-59-7

Synonyms:PFd9

分?式:C??H??D?Cl?FN?O

分?量:459.39

作?靶点:Isotope-LabeledCompounds

作?通路:Others

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性Crizotinib-d9(PFd9)是氘代标记的Crizotinib.Crizotinib(PF是?种具有?服活性的,

ATP竞争性的ALK和c-Met抑制剂,IC50分别为20和8nM。在细胞的实验中,Crizotinib抑制NPM-ALK的

酪氨酸磷酸化和c-Met的酪氨酸磷酸化,IC50分别为24和11nM。Crizotinib也是ROS1抑制剂。Crizotinib

具有有效的肿瘤?长抑制作?。

体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,

largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattention

becauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs.

REFERENCES

[1].RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019;53(2):211-

216.

McePd