EPZ-6438inhibitstheactivityofhumanPRC2-containingwild-typeEZH2withK_iof2.5±0.5nM.

Ki:2.5nM(EZH2)^[1]

EPZ-6438inhibitsEZH2inamannercompetitivewiththesubstrateS-adenosylmethionine(SAM).EPZ-6438inhibitsEZH1,EZH2(inpeptideassay),EZH2(innucleosomeassay)withIC₅₀of392nM,11nMand16nM,respectively.EPZ-6438displaysa35-foldselectivityversusEZH1and>4,500-foldselectivityrelativeto14otherHMTstested^[1].

EPZ-6438(125mg/kg)inducestumorstasisduringtheadmiNISTrationperiodandproducedasignificanttumorgrowthdelaycomparedwithvehicleafterthedosingperiod.MeasuringEPZ-6438plasmalevelseither5minbeforeor3hafterdosingonday21revealsacleardose-dependentincreaseinsystemicexposure^[1].Dose-dependenttargetinhibitionisobservedinPBMCsandbonemarrowfromratsdosedwithEPZ-6438(orallyadministered,100,300,or1,000mg/kg)asmeasuredbyELISA^[2].

• [1].KnutsonSK,etal.DurabletumorregressioningeneticallyalteredmalignantrhaBDoidtumorsbyinhibitionofmethyltransferaseEZH2.ProcNatlAcadSciUSA.2013May7;110(19):7922-7.

  [2].KnutsonSK,etal.SelectiveinhibitionofEZH2byEPZ-6438leadstopotentantitumoractivityinEZH2-mutantnon-Hodgkinlymphoma.MolCancerTher.2014Apr;13(4):842-54.

EPZ-6438isdissolvedinDMSOandstored,andthendilutedwithappropriatemediabeforeuse^[1].

293T(CRL-11268),RD(CRL-136),SJCRH30(CRL-2061),A204(HTB-82),G401(CRL-1441),G402(CRL-1440),KYM-1(JCRB0627),293T,RD,SJCRH30,A204,G401,andG402cellsareused.Onday0,cellsareeitheruntreated,DMSO-treated,ortreatedwithEPZ-6438startingat10µManddecreasingineitherthreefoldorfourfolddilutions.Platesarereadonday0,day4,andday7usingCellTiterGlo,withcompound/mediabeingreplenishedonday4.Onday7,thesix-wellplatesaretrypsinized,centrifuged,andresUSPendedinfreshmediaforcountingbyVi-Cell.Cellsfromeachtreatmentarereplatedattheoriginaldensityin96-wellplatesintriplicate.Cellsareallowedtoadheretotheplateovernight,andcellsaretreatedasonday0.Ondays7,11,and14,platesarereadusingCellTiterGlo,withcompound/mediabeingreplenishedonday11.Averagesoftriplicatesareusedtoplotproliferationoverthetimecourse,andcalculateIC₅₀values.Forcellcycleandapoptosis,G401andRDcellsareplatedin15-cmdishesinduplicateatadensityof1×10⁶cellsperplate.CellsareincubatedwithEPZ-6438at1µM,inatotalof25mL,overacourseof14d,withcellsbeingsplitbacktooriginalplatingdensityonday4,7,and11.CellcycleanalysisandTUNELassayareperformedusingaGuavaflowcytometer^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

EPZ-6438ispreparedin0.5%NaCMCplus0.1%Tween80inwater.

Mice^[1]
SCIDmicebearings.c.G401xenograftsareinoculateds.c.attherightflankwithG401tumorcells(5×10⁶cellspermouse)in0.2-mLmixtureofbasemediaandMatrigelfortumordevelopment.Thetreatmentsarestartedwhenthetumorsizereached157mm³forthetumorefficacystudy(n=16micepergroup).EPZ-6438(125mg/kg,250mg/kg,and500mg/kg)orvehicle(0.5%NaCMCplus0.1%Tween80inwater)isadministeredorallyBIDatadosevolumeof10µL/gforeither21or28d.Animalbodyweightsaremeasuredeverydayduringthefirstweek,andthentwiceweeklyfortheremainderofthestudy.Tumorsizeismeasuredtwiceweeklyintwodimensionsusingacaliper,andthevolumeisexpressedincubicmillimeters.
Rat^[2]
MaleandfemaleSprague-Dawleyrats(8weeksold)areorallytreatedwithEPZ-6438(100,300,or1,000mg/kg)orvehiclefor28daysonceaday.Onday22,thefemalesfromthehighestdosegroupreceivedanotherdoseandaresubsequentlyeuthanizedonday23approximately29hoursafterthelastdose.Allotheranimalsareeuthanizedonday29approximately29hoursafterthelastdoseadministeredonday28.Ateuthanasia,thefullbloodvolumeiscollected,peripheralbloodmononuclearcells(PBMC)areisolated,andcellpelletsarefrozenandstoredat−80°Cbeforeanalysis.A2-mm-thicksliceofskinisformalin-fixedfor24hoursandtransferredto70%ethanol.Thefixedtissuesareparaffinembedded.Bonemarrowsamplesarecollectedfromfemur,tibia,andhipbones,frozenandstoredat−80°Cbeforeanalysis.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].KnutsonSK,etal.DurabletumorregressioningeneticallyalteredmalignantrhabdoidtumorsbyinhibitionofmethyltransferaseEZH2.ProcNatlAcadSciUSA.2013May7;110(19):7922-7.

  [2].KnutsonSK,etal.SelectiveinhibitionofEZH2byEPZ-6438leadstopotentantitumoractivityinEZH2-mutantnon-Hodgkinlymphoma.MolCancerTher.2014Apr;13(4):842-54.

572.74

C₃₄H₄₄N₄O₄

1403254-99-8

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO:5.0mg/mL(needultrasonic)

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

Purity:99.63%

SelectBatch:HY-13803-23708HY-13803-25780HY-13803-26610HY-13803-23063HY-13803-15158HY-13803-16818HY-13803-23257HY-13803-10325HY-13803-15397HY-13803-24770HY-13803-25587HY-13803-23954HY-13803-25148HY-13803-23846HY-13803-23136HY-13803-23062HY-13803-22998HY-13803-10282HY-13803-17996

DataSheet(122KB)SDS(120KB)

COA(96KB)HNMR(341KB)LCMS(144KB)

HandlingInstructions(1252KB)

• [1].KnutsonSK,etal.DurabletumorregressioningeneticallyalteredmalignantrhabdoidtumorsbyinhibitionofmethyltransferaseEZH2.ProcNatlAcadSciUSA.2013May7;110(19):7922-7.

  [2].KnutsonSK,etal.SelectiveinhibitionofEZH2byEPZ-6438leadstopotentantitumoractivityinEZH2-mutantnon-Hodgkinlymphoma.MolCancerTher.2014Apr;13(4):842-54.

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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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