Anticancer-agent-207--生命科学试剂-MCE.pdf

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Inhibitors•ScreeningLibraries•Proteins

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Anticanceragent207

Cat.No.:HY-163515

分⼦式:C₂₉H₃₉FN₄O₂

分⼦量:494.64

作⽤靶点:Ras

作⽤通路:GPCR/GProtein;MAPK/ERKPathway

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性Anticanceragent207(compound10b)是⼀种有效的抗癌剂。Anticanceragent207与NRASrG4结合，KD

值为2.31µM。Anticanceragent207表现出细胞毒性并降低NRAS蛋⽩的表达。Anticanceragent207显⽰出

抗肿瘤活性[1]。

IC50TargetNRASrG4

2.31μM(Kd)

体外研究Anticanceragent207(48h)showscytotoxicityforNRAS-mutantmelanomaSK-MEL-2withanIC50valueof

2.0µM[1].

Anticanceragent207(0,0.5,1.0µM;72h)decreasestheexpressionofNRASprotein[1].

Anticanceragent207(0,0.13,0.25µM;10days)inhibitsthecolonyformationofSK-MEL-2cells[1].

WesternBlotAnalysis[1]

CellLine:SK-MEL-2cells

Concentration:0,0.5,1.0µM

IncubationTime:72h

Result:DecreasedtheexpressionofNRASproteininadose-dependentmanner.

CellProliferationAssay[1]

CellLine:MCF-7,HepG2,HL60,A375cells

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