1599440-33-1 Dxd DX-8951衍生物

CAS号 1599440-33-1

分子式 C26H24FN3O6

分子量 493.48

上海偶联医药科技有限公司，大量现货（qq 3193709336）

沸点 957.9±65.0°C(Predicted)

密度 1.57±0.1g/cm3(Predicted)

储存条件 Storeat-20°C

溶解度 DChemicalbookMSO:40.0(MaxConc.mg/mL);81.06(MaxConc.mM)

酸度系数 (pKa)11.18±0.40(Predicted)

用途 甲磺酸伊喜替康是一种DNA 拓扑异构酶 I (topoisomerase I) 抑制剂，IC50 值为 2.2 μM (0.975 μg/mL)，可用于癌症研究。

靶点 Topoisomerase I 0.31 μM (IC 50 ) Camptothecins

体外研究Dxd(ExatecanderivativeforADC)isapotentDNAtopoisomeraseIinhibitor,withanIC50of0.31μM,usedasaconjugateddrugofHER2-targetingADC(DS-8201a).DxdiscytotoxictohumancancercelllinesofKPL-4,NCI-N87,SK-BR-3,andMDA-MB-468withIC50sof1.43nM-4.07nM,butthecontrolIgG-ADC(Dxdisthepayload)showsnoinhibitiononthefourcelllines(withHER2expression).DS-8201a(Dxdisthepayload)displayssignifiChemicalbookcantsuppressionontheHER2-positiveKPL-4,NCI-N87,andSK-BR-3celllines,withIC50valuesof26.8,25.4,and6.7ng/mL,respectively,butwithnosuchinhibitiononMDA-MB-468(IC50,>10,000ng/mL).

体内研究

DS-8201a(Dxdisthepayload,10mg/kg,i.v.)showspotentantitumoractivityinHER2-positivemodelswithKPL4,JIMT-1,andCapan-1andinHER2low-expressingST565andST313modelswithHER2IHC1+/FISH-negativeexpression.