BRAFV600E-ABL2-IN-1-生命科学试剂-MCE.pdfVIP

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BRAFV600E/ABL2-IN-1

Cat.No.:HY-178382

分⼦式:C₂₄H₂₀BrClN₄O₃S

分⼦量:559.86

作⽤靶点:Raf;Bcr-Abl;P-glycoprotein;PERK;Apoptosis

作⽤通路:MAPK/ERKPathway;ProteinTyrosineKinase/RTK;

MembraneTransporter/IonChannel;CellCycle/DNADamage;

Apoptosis

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性BRAFV600E/ABL2-IN-1是⼀种BRAFV600E(IC50=0.088μM)/ABL2(IC50=0.3μM)双重抑制剂。

BRAFV600E/ABL2-IN-1可降低P-糖蛋⽩的表达。BRAFV600E/ABL2-IN-1可有效抑制A375-R⿊⾊素瘤细胞中

的p-CrkL(Abl2信号通路)和p-ERK1/2(BRAFV600E通路)。BRAFV600E/ABL2-IN-1可导致细胞周期停滞于

G1期，从⽽抑制细胞进⼊S期及后续各期以及G2/M期。BRAFV600E/ABL2-IN-1显著增加晚期凋亡(

apotosis)细胞的⽐例。BRAFV600E/ABL2-IN-1可⽤于⿊⾊素瘤的研究[1]。

IC50TargetBRafV600EBRafV600E

0.088μM(IC50)0.088μM(IC50)

体外研究BRAFV600E/ABL2-IN-1(Compound8h)(0.01-100μM,48h)exhibitsthebestactivitytowardsSK-MEL5

cellsatthemelanomapanel,withaGI50of0.54μM,demonstratingmarkedcytostaticactivityagainst

melanoma(SK-MEL-5;TGI=19.95μM)andcoloncancer(HT29;TGI=2