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Erlotinib-d8

Cat.No.:HY-50896S3

CASNo.:1266656-97-6

Synonyms:CP-358774-d;NSC718781-d;OSI-774-d

888

分?式:C??H??D?N?O?

分?量:401.49

作?靶点:Isotope-LabeledCompounds

作?通路:Others

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性Erlotinib-d8(CP-358774-d8)是氘代标记的Erlotinib.Erlotinib(CP-358774)是?种直接作?的EGFR酪氨酸激

酶抑制剂，对?EGFR的IC50为2nM。Erlotinib可降低完整肿瘤细胞的EGFR?磷酸化，IC50为20nM。

Erlotinib?于??细胞肺癌的研究。Erlotinib是?种点击化学试剂。它含有Alkyne基团，可以和含有Azide

基团的分?发?铜催化的叠氮-炔环加成反应(CuAAc)。

体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,

largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattention

becauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs.

REFERENCES

[1].RussakEM,etal.