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二盐酸奎吖因水合物 |
| CAS No.: |
69-05-6 |
| 分子式： |
C23H32Cl3N3O |
| 分子量： |
472.88 |
| 备注： |
中文名称二盐酸奎吖因水合物中文同义词疟疾平;二盐酸喹吖因;喹吖因二盐酸;阿的平二盐酸盐;二盐酸阿的平;二盐酸喹丫因;疟涤平;盐酸阿的平英文名称QUINACRINEDIHYDROCHLORIDE英文同义词6-CHLORO-9-(4-DIETHYLAMINO-1-METHYL-BUTYLAMINO)-2-METHOXYACRIDINEDIHYDROCHLORIDE;6-CHLORO-9-(4-DIETHYLAMINO-1-METHYL-N-BUTYL)AMINO-2-METHOXYACRIDINEDIHYDROCHLORIDE;ERIONHYDROCHLORIDE;DL-QUINACRINEHYDROCHLORIDE;CHINACRINHYDROCHLORIDE;CHEMIOCHINHYDROCHLORIDE;ARICHINHYDROCHLORIDE;ATABRINECAS号69-05-6分子式C23H32Cl3N3O分子量472.88EINECS号200-700-8相关类别小分子抑制剂;细胞信号和神经生物学;细胞生物学Mol文件69-05-6.mol结构式二盐酸奎吖因水合物性质熔点249-251℃(Decomposition)密度1.2962(roughestimate)折射率1.6300(estimate)储存条件+15Cto+30C溶解度可溶于DMSO（轻微）、甲醇（轻微、超声处理）、水（轻微）酸度系数(pKa)pKa-6.3(H2OtundefinedInotreportedbutlow)(Uncertain)形态黄色固体颜色浅黄色至厚黄色PH值3.0～5.0(20g/l,25℃)水溶解性Water:33.33mg/mL(70.48mM)Merck14,8044BRN4834013稳定性稳定的。与强氧化剂不相容。EPA化学物质信息Quinacrinehydrochloride(69-05-6)二盐酸奎吖因水合物用途与合成方法生物活性Quinacrine2HCl是具有多种作用的亲脂性阳离子药物，通常用作抗原生动物剂。Quinacrine是有效的phospholipaseA2抑制剂。靶点TargetValuePLA2()体外研究Quinacrine(5-20μM;24hours)inhibitsthegrowthofSGC-7901cells.Quinacrine(7.5and15μM;24hours)inducesapoptosisinSGC-7901cells,whichisassociatedwithmitochondria-dependentsignalpathwayandinvolvesp53upregulationandcaspase-3activationpathway.Quinacrine(15μM;24hours)treatmentsignificantlyincreasedthelevelsofproapoptoticproteins,includingcytochromec,Bax,andp53,anddecreasedthelevelsofantiapoptoticproteinBcl-2,thusshiftingtheratioofBax/Bcl-2infavorofapoptosis.CellViabilityAssayCellLine:SGC-7901cellsConcentratChemicalbookion:0,5,10,15,and20μMIncubationTime:24hoursResult:Cellviabilitywasinhibitedinadose-dependentmanner,andthemeanIC50valueis16.18μM.ApoptosisAnalysisCellLine:SGC-7901cellsConcentration:7.5and15μMIncubationTime:24hoursResult:Thepercentageofapoptoticcells,includingtheearlyphaseandlatephaseapoptosis,increasedto26.30%,comparedwithcontrolgroupof3.37%.WesternBlotAnalysisCellLine:SGC-7901cellsConcentration:15μMIncubationTime:24hoursResult:Therelativequantityofcytochromecproteinwasupregulated,increasedfrom0.10to0.24.Therelativequantityofp53proteinwasdramaticallyincreased,from0.06to0.19.TheBax/Bcl-2ratiowasdramaticallyelevatedfrom1.21to2.59.体内研究Quinacrine(100mg/kgthreetimesperweekfortwoconsecutiveweeks)significantlysuppressescirculatingblastcellsatdays30/31andincreasesthemediansurvivaltime(MST).Quinacrinedoesnotdecreasethebodyweightoftreatedanimalsatthetesteddose.AnimalModel:FemaleSCIDmicewithacutemyeloidleukemia(AML)-PSmodelDosage:100mg/kgAdministration:Administeredbyoralgavage(po);threetimesaweekfortwoconsecutiveweeksResult:InthefirstAMLmouseinvivostudy,evaluationofcirculatingleukemiccellsdetectedinbloodsamples(inpercentofwhitebloodcells(WBC))atday30/31showed72%humantumorcellsinthecontrolmice,whereasinmicetreatedwithQuinacrine,thiswasonly2.2%.TheMSTofcontrolmicewas34dayswhereasitwas46daysinQuinacrine-treatedmice.类别有毒物质毒性分级中毒急性毒性口服-大鼠LD50:660毫克/公斤;口服-小鼠LD50:557毫克/公斤可燃性危险特性可燃;火场释放有毒氮氧化物,氯化物烟雾储运特性库房低温,通风,干燥灭火剂水,二氧化碳,泡沫,沙土 |
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