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二鹽酸奎吖因水合物 |
| CAS No.: |
69-05-6 |
| 分子式： |
C23H32Cl3N3O |
| 分子量： |
472.88 |
| 備注： |
中文名稱二鹽酸奎吖因水合物中文同義詞瘧疾平;二鹽酸喹吖因;喹吖因二鹽酸;阿的平二鹽酸鹽;二鹽酸阿的平;二鹽酸喹丫因;瘧滌平;鹽酸阿的平英文名稱QUINACRINEDIHYDROCHLORIDE英文同義詞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號69-05-6分子式C23H32Cl3N3O分子量472.88EINECS號200-700-8相關類別小分子抑制劑;細胞信號和神經(jīng)生物學;細胞生物學Mol文件69-05-6.mol結構式二鹽酸奎吖因水合物性質熔點249-251℃(Decomposition)密度1.2962(roughestimate)折射率1.6300(estimate)儲存條件+15Cto+30C溶解度可溶于DMSO（輕微）、甲醇（輕微、超聲處理）、水（輕微）酸度系數(shù)(pKa)pKa-6.3(H2OtundefinedInotreportedbutlow)(Uncertain)形態(tài)黃色固體顏色淺黃色至厚黃色PH值3.0～5.0(20g/l,25℃)水溶解性Water:33.33mg/mL(70.48mM)Merck14,8044BRN4834013穩(wěn)定性穩(wěn)定的。與強氧化劑不相容。EPA化學物質信息Quinacrinehydrochloride(69-05-6)二鹽酸奎吖因水合物用途與合成方法生物活性Quinacrine2HCl是具有多種作用的親脂性陽離子藥物，通常用作抗原生動物劑。Quinacrine是有效的phospholipaseA2抑制劑。靶點TargetValuePLA2()體外研究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.體內研究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.類別有毒物質毒性分級中毒急性毒性口服-大鼠LD50:660毫克/公斤;口服-小鼠LD50:557毫克/公斤可燃性危險特性可燃;火場釋放有毒氮氧化物,氯化物煙霧儲運特性庫房低溫,通風,干燥滅火劑水,二氧化碳,泡沫,沙土 |
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