169869-90-3 甲磺酸伊喜替康

中文名称 甲磺酸伊喜替康

英文名称 Exatecan mesilate

上海偶联医药科技有限公司 kg+库存，可供GMP级

CAS号 169869-90-3

分子式C25H26FN3O7S

分子量531.56

储存条件 4°C, protect from light, stored under nitrogen

溶解度DMSO:7.41(MaxConc.mg/mL);13.94(MaxConc.mM)Water:0.0Chemicalbook(MaxConc.mg/mL);0.19(MaxConc.mM)

形态Asolid

稳定性Hygroscopic

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

生物活性 Exatecanmesylate(DX895Chemicalbook1f)是一种DNA拓扑异构酶I(topoisomeraseI)抑制剂，IC50值为2.2μM(0.975μg/mL)，可用于癌症研究。

靶点 TopoisomeraseI0.975μg/mL(IC50)

体外研究ExatecanmesylateisapotenttopoisomeraseIinhibitor,withanIC50of0.975μg/mL.Exatecanmesylate(DX-8951f)significantlyinhibitstheproliferationofseveralcancercelllines,withmeanGI50sof2.02ng/mL,2.92ng/mL,1.53ng/mL,and0.877ng/mLforbreastcancercells,coloncancercells,stomachcancercellsandlungcancercells,respectively.Exatecanmesylate(DX-8951f)displayscytotoxicactivitiesagainstPC-6,PC-6/SN2-5cells,withmeanGI50sof0.186and0.395ng/mL,respctively.Exatecanmesylate(34nM)stabiliChemicalbookzesDNA-TopoIcomplexesinPC-6andPC-6/SN2-5cells.

体内研究Exatecanmesylate(DX-8951f,3.325-50mg/kg,i.v.)exhibitsantitumoractivitiesinthemicemodelbearingtumorcells,withouttoxicdeath.Exatecanmesylate(15,25mg/kg,i.v.)hightlyinhibitsMIA-PaCa,BxPC-3primarytumorgrowthintheMIA-PaCa-2early-stagemodelandearly-stagemodelofBxPC-3.Exatecanmesylate(15,25mg/kg,i.v.)alsosignificantlysuppressesBxPC-3lymphaticmetastasisandcompletelyeliminateslungmetastasisintheBxPC-3late-stagecancermodel.