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文件名称:Rovalpituzumab-tesirine-SC-002-生命科学试剂-MCE.pdf
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文档摘要

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Inhibitors?ScreeningLibraries?Proteins

www.MedChemE

Rovalpituzumabtesirine

Cat.No.:HY-132257

CASNo.:1613313-09-9

Synonyms:SC-002

作?靶点:Antibody-DrugConjugates(ADCs);Notch

作?通路:Antibody-drugConjugate/ADCRelated;NeuronalSignaling;

StemCell/Wnt

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性Rovalpituzumabtesirine(SC-002)是?种具有抗癌作?的抗体-药物偶联物(ADC)。Rovalpituzumabtesirine

包含靶向DLL3的抗体Rovalpituzumab(HY-P99043),该抗体通过蛋?酶可裂解的连接体与细胞毒药物吡咯

并苯?氮卓类化合物连接。Rovalpituzumabtesirine可?于?细胞肺癌(SCLC)的研究。

体外研究Rovalpituzumabtesirine(0.01-10000pM,96h)caneffectivelybindtomiceDLL3inKP1cells(SCLCmodel)

expressingmiceDLL3,exhibitingpotentkillingeffectsandexertingcytotoxicitythroughinternalizationofPBD

toxin[2].

体内研究Rovalpituzumabtesirine(0.03,0.1,0.3mg/kg,i.p.onedose)inhibitestumorgrowthinadose-dependent

mannerintheSCLCmicemodel,andthe0.3mg/kggroupachievescompleteremission,theanti-tumor

effectismoresignificantwhencombineswithanti-PD1[2].

Rovalpituzumabtesirine(0.03mg/kg,i.ponceeveryfourdays)combineswithanti-PD1intheSCLCmice