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Inhibitors?ScreeningLibraries?Proteins
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Clifutinib
Cat.No.:HY-172581
CASNo.:1862226-99-0
分?式:C??H??N?O?
分?量:502.6
作?靶点:FLT3;Apoptosis;Ras;p38MAPK;PI3K;Akt;JAK;STAT
作?通路:ProteinTyrosineKinase/RTK;Apoptosis;GPCR/GProtein;
MAPK/ERKPathway;PI3K/Akt/mTOR;Epigenetics;
JAK/STATSignaling;StemCell/Wnt
储存?式:Pleasestoretheproductundertherecommendedconditionsin
theCertificateofAnalysis.
BIOLOGICALACTIVITY
?物活性Clifutinib(Compound9e)是?种具有?服活性的选择性的FMS样酪氨酸激酶3(FLT3-ITD)内部串联重复突变
抑制剂,IC50值为15.1nM。Clifutinib抑制FLT3-ITD激酶活性,阻断FLT3下游RAS/MAPK、PI3K/AKT和
JAK/STAT5信号通路。Clifutinib诱导FLT3-ITD突变的急性髓系??病(AML)细胞凋亡(apoptosis)。
Clifutinib有望?于复发/难治性FLT3-ITD阳性急性髓系??病的研究[1]。
REFERENCES
[1].LiuB,etal.DiscoveryofFLT3-ITDInhibitorClifutinib:ANovelBiphenylacetyleneUreaDerivativeinClinicalTrialsfortheTreatmentof
Relapsed/RefractoryFLT3-ITD+AcuteMyeloidLeukemia.JMedChem.2025Apr24;68(8):7955-7972.
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