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RGN6024

Cat.No.:HY-176537

CASNo.:3055038-20-2

分⼦式:C₁₈H₂₁N₅O₄S

分⼦量:403.46

作⽤靶点:Microtubule/Tubulin

作⽤通路:CellCycle/DNADamage;Cytoskeleton

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性RGN6024是⼀种可透过⾎脑屏障的、具有⼝服活性且可逆的⼩分⼦微管蛋⽩(tubulin)去稳定剂。RGN6024

在⽣化和细胞实验中均能抑制微管聚合，与β-微管蛋⽩的秋⽔仙碱结合⼝袋结合(SPR:Kd=6.7μ

M；tryptophanassay:Kd=7.4μM)，并在胶质母细胞瘤(GB)细胞中触发G2/M期阻滞。RGN6024在βIII-

微管蛋⽩过表达的细胞中仍保持活性。RGN6024在胶质母细胞瘤(GB)异种移植⼩⿏模型中可抑制肿瘤⽣长。

RGN6024可⽤于胶质母细胞瘤(GB)的研究[1]。

体外研究RGN6024(100nM,48h)bindstothecolchicinebindingsiteofβ-tubulinanddisruptsmicrotubule

morphologyinU87glioblastomacells[1].

RGN6024(72h)reversiblydecreasestheviabilityofglioblastomacellswithIC50valuesof85nM(U87),23

nM(LN-18)and120nM(BT142)[1].

RGN6024(0.001-100μM,6h)demonstrateshighreversibilityinU87cellviabilitywashoutexperiments,with

anIC50of2482nMafterwashout(30-foldshiftfrom81.6nMno-washout)[1].

RGN6024(250nM,48h)inducesG2/MarrestinU87cellsandisnotsusceptibletoβIII-tubulin