Hotline:400-820-3792

Inhibitors?ScreeningLibraries?Proteins

www.MedChemE

PDGFRαkinaseinhibitor3

Cat.No.:HY-173275

分?式:C??H??N?O

分?量:385.46

作?靶点:PDGFR

作?通路:ProteinTyrosineKinase/RTK

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性PDGFRαkinaseinhibitor3(CompoundL7)是?种靶向PDGFRαD842V激酶的强效抑制剂，在?化和细胞分

析中的IC50值分别为23.8nM和2.1nM。PDGFRαkinaseinhibitor3与PDGFRαD842V的ATP结合位点结

合，从?阻断其下游信号通路并抑制激酶活性。PDGFRαkinaseinhibitor3可?于胃肠道间质瘤(GIST)的研

究[1]。

IC50TargetIC50:PDGFRαD842V/G680R(64.1nM),PDGFRαD842V/T674I(27.6nM)

REFERENCES

[1].LiangH,etal.DesigningMacrocyclicKinaseInhibitorsUsingMacrocycleScaffoldHoppingwithReinforcedLearning(Macro-Hop).J

MedChem.2025Mar27;68(6):6698-6717.

McePdfHeight

Caution:Producthasnotbeenfullyvalidatedformedicalapplications.

Forresearchuseonly.

Tel:400-820-3792;021Fax:021E-mail:tech@MedChemE

1/1