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Inhibitors?ScreeningLibraries?Proteins
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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