DTS-201-sodium-生命科学试剂-MCE.pdf

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DTS-201sodium

Cat.No.:HY-P10759

CASNo.:372491-73-1

分⼦式:C₄₉H₆₄N₅NaO₁₈

分⼦量:1034.04

作⽤靶点:Aminopeptidase

作⽤通路:MetabolicEnzyme/Protease

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性DTS-201sodium(CPI-0004Na)是⼀种Doxorubicin(HY-15142A)的肽前药。DTS-201包括四肽部分，在肿瘤

环境中被内肽酶⽔解产⽣代谢物，继⽽进⼊细胞后转化为活性Doxorubicin。DTS-201在前列腺癌、乳腺癌和

肺癌的肿瘤异种移植模型中显⽰出抗肿瘤疗效[1]。

体内研究DTS-201(40-100mg/kginmice,30-70mg/kginrats,and4-8mg/kgindogs,i.v.,15min)iswelltoleratedin

mice,rats,anddogs[1].

DTS-201(i.v.,15min,onday1and22)iswelltoleratedinmice(50mg/kg,MTD)andrats(40mg/kg,MTD)

[1].

DTS-201(3.2,12.8and25.6mg/kg,i.v.,onceweeklyfor7weeks)showslesscardiotoxicitythanDoxorubicin

[1].

DTS-201(40-80mg/kg,i.v.)hasabettertherapeuticindexthanfreeDoxorubicininNCI-H1299,PC-3,and

MDA-MB-231xenograftmice[1].

ToxicokineticvariablesofDTS-201inBeagledogsaftera15-minintravenousinfusionofDTS-201at

increasingdoselevelshERGIC50Dose(mg/kg)D