Cisplatinisapotentinducerofgrowtharrestand/orapoptosisinmostcelltypes.

Apoptosisinducer^[1]

Cisplatin(CDDP)causesapoptosisofHeLacellsinadose-dependentmanner,withaconcentrationof30μMCisplatinresultingindeathofgreaterthan90%ofthecellpopulationby24hoftreatment.ThekineticsofCisplatin-inducedapoptosisareexaminedusinga30μMconcentration.CisplatinActivatestheMEK/ERKSignalingPathway,20and30μMCisplatin,bothofwhichresultsinsignificantapoptosis,leadstostrongactivationofERK^[1].Cisplatin(50μM)producestime-dependentapoptosisinrenalproximaltubularcell(RPTCs),causingcellshrinkage,a50-foldincreaseincaspase3activity,a4-foldincreaseinphosphatidylserineexternalization,and5-and15-foldincreasesinchromatincondensationandDNAhypoploidy,respectively^[2].

Inmelanoma-bearingmice,Cisplatin(4mg/kgB.W.)reducesthesizeandweightofthesolidtumors,andHemoHIMsupplementationwithCisplatinenhancesthedecreaseofboththetumorsizeandweight^[3].CisplatinadmiNISTrationresultsinsignificantincreasesinthekidneyweightasapercentageofthetotalbodyweight,urinevolume,serumcreatinine,andbloodureanitrogenbyabout132,315,797,and556%incomparisonwiththecontrolrats,respectively^[4].

• [1].WangX,etal.RequirementforERKactivationincisplatin-inducedapoptosis.JBiolChem.2000Dec15;275(50):39435-43.

  [2].CummingsBS,etal.Cisplatin-inducedrenalcellapoptosis:caspase3-dependentand-independentpathways.JPharmacolExpTher.2002Jul;302(1):8-17.

  [3].ParkHR,etal.EnhancedantitumorefficacyofcisplatinincombinationwithHemoHIMintumor-bearingmice.BMCCancer.2009Mar17;9:85.

  [4].ShimedaY,etal.Protectiveeffectsofcapsaicinagainstcisplatin-inducednephrotoxicityinrats.BiolPharmBull.2005Sep;28(9):1635-8.

  [5].HallMD,etal.SaynotoDMSO:dimethylsulfoxideinactivatescisplatin,carboplatin,andotherplatinumcomplexes.CancerRes.2014Jul15;74(14):3913-22.

CisplatinisdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse^[1].

HeLaandA549cellsaremaintainedinDulbecco"smodifiedEagle"smediumsupplementedwith10%fetalbovineserum,100unitsofPenicillin,and100μgofStreptomycin/mL.Theyareculturedat37°Cinahumidifiedchambercontaining5%CO₂.Fortheinductionofapoptosis,cellsareplatedin60-mmdishes1daypriortoCisplatin(0-30μM)treatment^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

Cisplatinispreparedinwater(Mice)^[3].
Cisplatinispreparedinphysiologicalsalinesolution(Rat)^[4].

Mice^[3]
Micearedividedrandomlyintothreegroups(Control,CisplatinandCisplatin+HemoHIM),andeachgroupconsistsoftwentymice.B16F0melanoma(5×10⁵cells/mouse)isinoculatedintosubcutaneousfemoralleftregionofmiceat3daysbeforeaninitialinjectionofCisplatin.Cisplatinisinjectedintraperitoneallyat4mg/kgbodyweight(B.W.)onday0,7and14(totalthreeinjections).ExperimentalgroupisintubatedwithHemoHIMatafinalconcentrationof100mg/kgB.W.byeverydayfromday-1today16,whilethecontrolgroupreceivedonlywater.Onday17afterinitialinjectionofCisplatin,allmiceofeachgroupareexperimented,respectively,toevaluatetumorweightortumorsize.Thetumorsizeiscalculatedasfollows:tumorsize=ab²/2,whereaandbarethelargerandsmallerdiameters,respectively.
Rat^[4]
MaleSprague-Dawleyratsweighing200to250garedividedatrandominto4groupsof4or5animalseach.Thefirstgroup(control)receivedavehicle(5%carboxymethylcellulosesodiumsolution(CMC-Na),5mL/kgbodywt.,p.o.)usedforCapsaicin(Cap).ThesecondgroupreceivedCap(10mg/kg/d,p.o.)in5%CMC-Na(5mL/kg),andthethirdreceived5%CMC-Nafor6consecutivedaysinjectedwithCisplatin(5mg/kginphysiologicalsalinesolution,i.p.).ThefourthgroupreceivedCap(10mg/kg/d,p.o.)in5%CMC-Nafor6consecutivedaysafterCisplatininjection(5mg/kg,i.p.).Forallgroups,Caporvehicleisgiventwicedaily.TheselectedCapconcentrationandthedoseadministrationschedulewithoutinducinganyratintestinaldamagearechosenusingdatafromourpreliminaryexperiments.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].WangX,etal.RequirementforERKactivationincisplatin-inducedapoptosis.JBiolChem.2000Dec15;275(50):39435-43.

  [2].CummingsBS,etal.Cisplatin-inducedrenalcellapoptosis:caspase3-dependentand-independentpathways.JPharmacolExpTher.2002Jul;302(1):8-17.

  [3].ParkHR,etal.EnhancedantitumorefficacyofcisplatinincombinationwithHemoHIMintumor-bearingmice.BMCCancer.2009Mar17;9:85.

  [4].ShimedaY,etal.Protectiveeffectsofcapsaicinagainstcisplatin-inducednephrotoxicityinrats.BiolPharmBull.2005Sep;28(9):1635-8.

  [5].HallMD,etal.SaynotoDMSO:dimethylsulfoxideinactivatescisplatin,carboplatin,andotherplatinumcomplexes.CancerRes.2014Jul15;74(14):3913-22.

300.05

Cl₂H₆N₂Pt

15663-27-1

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO:≥31mg/mL(DMSOcaninactivateCisplatin"sactivity;pleaseseethereference[5]).

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:>98.00%

SelectBatch:HY-17394-13241HY-17394-16704HY-17394-27280HY-17394-26477HY-17394-25276HY-17394-24464HY-17394-21651HY-17394-19490

DataSheet(120KB)SDS(579KB)

COA(91KB)HNMR(238KB)

HandlingInstructions(1252KB)

• [1].WangX,etal.RequirementforERKactivationincisplatin-inducedapoptosis.JBiolChem.2000Dec15;275(50):39435-43.

  [2].CummingsBS,etal.Cisplatin-inducedrenalcellapoptosis:caspase3-dependentand-independentpathways.JPharmacolExpTher.2002Jul;302(1):8-17.

  [3].ParkHR,etal.EnhancedantitumorefficacyofcisplatinincombinationwithHemoHIMintumor-bearingmice.BMCCancer.2009Mar17;9:85.

  [4].ShimedaY,etal.Protectiveeffectsofcapsaicinagainstcisplatin-inducednephrotoxicityinrats.BiolPharmBull.2005Sep;28(9):1635-8.

  [5].HallMD,etal.SaynotoDMSO:dimethylsulfoxideinactivatescisplatin,carboplatin,andotherplatinumcomplexes.CancerRes.2014Jul15;74(14):3913-22.

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托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-Tropanylindole-3-carboxylate;lαH，5Αh-Tropan-3α-ylindole-3-carboxylate中文名称:托烷司琼中文同义词:托普西隆;托普西龙;曲匹西龙;托烷司琼;Β-托烷司琼;CS-348;Β-内托烷司琼;吲哚-3-甲酰氯;Β-托烷司琼(光学异构体);Β-托烷司琼,托烷司琼异构体CBNumber:CB3236404分子式:C17H20N2O2分子量:284.35MOLFile:89565-68-4.mol化学性质安全信息用途供应商112化学性质安全信息用途供应商112托烷司琼化学性质熔点:201-202°C沸点:448.5±35.0°C(Predicted)密度:1.26储存条件:2-8°C溶解度:H2O:soluble形态:solid酸度系数(pKa):15.38±0.30(Predicted)颜色:whiteCAS数据库:Chemicalbook89565-68-4(CASDataBaseReference)安全信息WGKGermany:3托烷司琼化学药品说明书托烷司琼|药物应用信息托烷司琼性质、用途与生产工艺临床评价Sorbe等报道本品对含顺铂(剂量50～89mg/m2)化疗方案引起的急性呕吐完全控制率为63%。58例恶性肿瘤化疗所致恶心、呕吐者，应用托烷司琼或昂丹司琼8mg分别在同一病人前后2个化疗周期的第1d给药前30min静脉注射，并用地塞米松10mg静脉滴注。结果两药控制急性及迟发性恶心、呕吐的疗效基本相似，均可达81%～100%。本品对强致吐化疗药物顺铂的止吐疗效突出。药物相关作用饮食可略为延长本品的吸收。本品与利福平、苯巴比妥等肝酶诱导药同时使用，可加快代谢，故快代谢型者需增加剂量，慢者则不必。西咪替丁等肝酶抑制药对本品血药浓度无明显影响。适应症托烷司琼临床用于预防和治疗癌症化疗引起的恶心和呕吐。化学性质结晶，熔点201-202℃(二氯甲烷-乙酸乙酯)。单盐酸托烷司琼(TropisetronMonohydroehloride)：C17H20N2O2?HCI。[105826-92-4]。熔点283-285℃(分解)。用途有高效性和选择性的5-HT3受体拮抗剂。用于化疗所致的呕吐。用途为5-羟色胺拮抗药生产方法托品醇(I)和酰氯(Ⅱ)反应，可得托烷司琼。托烷司琼上下游产品信息上游原料托品醇下游产品

公司介绍

托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-

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