PROTAC-c-Met-degrader-1-生命科学试剂-MCE.pdf

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PROTACc-Metdegrader-1

Cat.No.:HY-168135

CASNo.:3056647-52-7

分⼦式:C₄₅H₄₁FN₁₀O₅

分⼦量:820.87

作⽤靶点:PROTACs;c-Met/HGFR

作⽤通路:PROTAC;ProteinTyrosineKinase/RTK

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性PROTACc-Metdegrader-1(CompoundMet-DD4)是⼝服有效的PROTAC降解剂，对c-Met的DC50为6.21

nM。PROTACc-Metdegrader-1抑制c-Met成瘾细胞MKN-45的增殖，IC50为4.37nM，并在G0/G1期阻滞

细胞周期。PROTACc-Metdegrader-1在MKN-45异种移植⼩⿏模型中表现出抗肿瘤活性。(粉⾊：靶蛋⽩配

体(HY-13404)；蓝⾊：E3连接酶配体(HY-W087383)；⿊⾊：连接⼦(HY-W074901))

IC50Targetc-Met

6.21nM(DC50)

REFERENCES

[1].YingS,etal.,SelectiveandOrallyBioavailablec-MetPROTACsfortheTreatmentofc-Met-AddictedCancer.JMedChem.2024Oct

10;67(19):17053-17069.

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Caution:Producthasnotbeenfullyvalidatedformedicalapplications.

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