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BSJ-04-146

Cat.No.:HY-179512

CASNo.:2414478-45-6

分⼦式:C₅₀H₅₇F₃N₈O₈

分⼦量:955.03

作⽤靶点:PROTACs;FAK

作⽤通路:PROTAC;ProteinTyrosineKinase/RTK

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性BSJ-04-146是⼀种⾼效且选择性的PROTAC靶向黏着斑激酶(FAK)(IC50=26nM)。BSJ-04-146可在癌细胞中

快速有效地降解FAK，且具有⾼度的蛋⽩质组特异性，并在⼩⿏体内诱导持久降解。BSJ-04-146与FAK结合

，并需要泛素-蛋⽩酶体系统才能实现FAK的降解。BSJ-04-146可⽤于胰腺癌和三阴性乳腺癌的研究[1]。

体外研究BSJ-04-146(1-1000nM,4h)canefficientlydegradeFAKproteininPATU-8988Tcells[1].

BSJ-04-146(100nM,1-24h)canrapidlyinduceFAKdegradationinPATU-8988Tcellsandsimultaneously

significantlyreducepAKTsignaling[1].

BSJ-04-146(120h)significantlyinhibitsthe3DspheroidviabilityofPATU-8988TandMDA-MB-231cells[1].

BSJ-04-146(100nM,4-24h)inducedsignificantchangesin74pYand161pY-IMACphosphopeptidesin

PATU-8988Tcells(includingdownregulationofFAKautophosphorylationsites);thechangespersistedafter

24hoursoftreatment[1].

WesternBlotAnalysis[1]

CellLine:PATU-8988Tcells

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