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公司介绍
MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务。 MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌

MedKoo Biosciences/MRK003/205885/1g

MedKoo Biosciences/MRK003/205885/1g
  • MedKoo Biosciences/MRK003/205885/1g
商品介绍
MRK003isaγ-secretaseinhibitorexhibitspromisinginvitropre-clinicalactivityinmultiplemyelomaandnon-Hodgkin"slymphoma.MRK003treatmentinducedcaspase-dependentapoptosisandinhibitedproliferationofMMandNHLcelllinesandpatientcells.Examinationofsignalingeventsaftertreatmentshowedtime-dependentdecreaseinlevelsofthenotchintracellulardomain,Hes1andc-Myc.MRK003downregulatedcyclinD1,Bcl-XlandXiaplevelsinNHLcellsandp21,Bcl-2andBcl-XlinMMcells.Inaddition,MRK003causedanupregulationofpAkt,indicatingcrosstalkwiththePI3K/Aktpathway.

MedKooCat#:205885
Name:MRK003
CAS#:623165-93-5
ChemicalFormula:C25H31F6N3O2S
ExactMass:551.20412
MolecularWeight:551.59
ElementalAnalysis:C,54.44;H,5.66;F,20.67;N,7.62;O,5.80;S,5.81


Synonym:MRK003;MRK003;MRK-003.

IUPAC/ChemicalName:(3"R,6R,9R)-5"-(2,2,2-trifluoroethyl)-2-((E)-3-(4-(trifluoromethyl)piperidin-1-yl)prop-1-en-1-yl)-5,6,7,8,9,10-hexahydrospiro[6,9-methanobenzo[8]annulene-11,3"-[1,2,5]thiADIazolidine]1",1"-dioxide.

InChiKey:NKHUILHBYOOZDF-RWIQBJEJSA-N

InChiCode:InChI=1S/C25H31F6N3O2S/c26-24(27,28)16-34-15-23(32-37(34,35)36)21-5-6-22(23)14-19-12-17(3-4-18(19)13-21)2-1-9-33-10-7-20(8-11-33)25(29,30)31/h1-4,12,20-22,32H,5-11,13-16H2/b2-1+/t21-,22-,23-/m1/s1

SMILESCode:FC(C1CCN(C/C=C/C2=CC=C3C(C[C@@]4([H])CC[C@]([C@@]4(CN5CC(F)(F)F)NS5(=O)=O)([H])C3)=C2)CC1)(F)F


TechnicalData

Appearance:
Solidpowder

Purity:
>98%(orrefertotheCertificateofAnalysis)

ShippingCondition:
Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.

StorageCondition:
Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).

Solubility:
SolubleinDMSO,notinwater

ShelfLife:
>2yearsifstoredproperly

DrugFormulation:
ThisdrugmaybeformulatedinDMSO

StockSolutionStorage:
0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).

HarmonizedSystemCode:
293490


AdditionalInformation

 
 
Highlightsofrecentresearchusingthisagent
 MRK-003inhibitsNotch4signaling,growth,andapoptosisoflungcancercelllinesinvitroandinvivousingmousexenograftmodels (CancerRes2007;67(17):8051–7,http://cancerres.aacrjournals.org/content/67/17/8051.full).
 
 
 


References

1:TanakaS,NakadaM,YamadaD,NakanoI,TodoT,InoY,HoshiiT,TadokoroY,OhtaK,AliMA,HayashiY,HamadaJ,HiraoA.Strongtherapeuticpotentialofγ-secretaseinhibitorMRK003forCD44-highandCD133-lowglioblastomainitiatingcells.JNeurooncol.2015Jan;121(2):239-50.doi:10.1007/s11060-014-1630-z.Epub2014Oct8.PubMedPMID:25293440.

2:StoeckA,LejnineS,TruongA,PanL,WangH,ZangC,YuanJ,WareC,MacLeanJ,Garrett-EngelePW,KlukM,LaskeyJ,HainesBB,MoskalukC,ZawelL,FawellS,GillilandG,ZhangT,KremerBE,KnoechelB,BernsteinBE,PearWS,LiuXS,AsterJC,SathyanarayananS.DiscoveryofbioMarkerspredictiveofGSIresponseintriple-negativebreastcancerandadenoidcysticcarcinoma.CancerDiscov.2014Oct;4(10):1154-67.doi:10.1158/2159-8290.CD-13-0830.Epub2014Aug7.PubMedPMID:25104330;PubMedCentralPMCID:PMC4184927.

3:GroenewegJW,DiGloriaCM,YuanJ,RichardsonWS,GrowdonWB,SathyanarayananS,FosterR,RuedaBR.InhibitionofnotchsignalingincombinationwithPaclitaxelreducesplatinum-resistantovariantumorgrowth.FrontOncol.2014Jul7;4:171.doi:10.3389/fonc.2014.00171.eCollection2014.PubMedPMID:25072022;PubMedCentralPMCID:PMC4083224.

4:SamoreWR,GondiCS.Briefoverviewofselectedapproachesintargetingpancreaticadenocarcinoma.ExpertOpinInvestigDrugs.2014Jun;23(6):793-807.doi:10.1517/13543784.2014.902933.Epub2014Mar27.Review.PubMedPMID:24673265.

5:GroenewegJW,HallTR,ZhangL,KimM,ByronVF,TambouretR,SathayanrayananS,FosterR,RuedaBR,GrowdonWB.Inhibitionofgamma-secretaseactivityimpedesuterineSEROuscarcinomagrowthinahumanxenograftmodel.GynecolOncol.2014Jun;133(3):607-15.doi:10.1016/j.ygyno.2014.03.560.Epub2014Mar22.PubMedPMID:24667249.

6:LiuQQ,LiuJL,GuoDM,TengQL.[Inhibitoryeffectsofgammasecretaseinhibitoronhumanmultiplemyelomaxenograftmousemodel].ZhonghuaXueYeXueZaZhi.2013Sep;34(9):794-7.doi:10.3760/cma.j.issn.0253-2727.2013.09.012.Chinese.PubMedPMID:24103879.

7:TimmeCR,GruidlM,YeatmanTJ.Gamma-secretaseinhibitionattenuatesoxaliplatin-inducedapoptosisthroughincreasedMcl-1and/orBcl-xLinhumancoloncancercells.Apoptosis.2013Oct;18(10):1163-74.doi:10.1007/s10495-013-0883-x.PubMedPMID:23887890.

8:ChuQ,OrrBA,SemenkowS,BarEE,EberhartCG.ProlongedinhibitionofglioblastomaxenograftinitiationandclonogenicgrowthfollowinginvivoNotchblockade.ClinCancerRes.2013Jun15;19(12):3224-33.doi:10.1158/1078-0432.CCR-12-2119.Epub2013Apr29.PubMedPMID:23630166;PubMedCentralPMCID:PMC3686970.

9:HassanKA,WangL,KorkayaH,ChenG,MaillardI,BeerDG,KalemkerianGP,WichaMS.Notchpathwayactivityidentifiescellswithcancerstemcell-likepropertiesandcorrelateswithworsesurvivalinlungadenocarcinoma.ClinCancerRes.2013Apr15;19(8):1972-80.doi:10.1158/1078-0432.CCR-12-0370.Epub2013Feb26.PubMedPMID:23444212;PubMedCentralPMCID:PMC3630232.

10:JinR,NakadaM,TengL,FurutaT,SABItH,HayashiY,DemuthT,HiraoA,SatoH,ZhaoG,HamadaJ.CombinationtherapyusingNotchandAktinhibitorsiseffectiveforsuppressinginvasionbutnotproliferationingliomacells.NeurosciLett.2013Feb8;534:316-21.doi:10.1016/j.neulet.2012.12.008.Epub2012Dec20.PubMedPMID:23262078.

11:LiangS,GalluzzoP,SobolA,SkuchaS,RamboB,BocchettaM.MultimodalityApproachestoTreatHypoxicNon-SmallCellLungCancer(NSCLC)Microenvironment.GenesCancer.2012Feb;3(2):141-51.doi:10.1177/1947601912457025.PubMedPMID:23050046;PubMedCentralPMCID:PMC3463922.

12:MizumaM,RasheedZA,YabuuchiS,OmuraN,CampbellNR,deWildeRF,DeOliveiraE,ZhangQ,PuigO,MatsuiW,HidalgoM,MaitraA,RajeshkumarNV.ThegammasecretaseinhibitorMRK-003attenuatespancreaticcancergrowthinpreclinicalmodels.MolCancerTher.2012Sep;11(9):1999-2009.doi:10.1158/1535-7163.MCT-12-0017.Epub2012Jul2.PubMedPMID:22752426;PubMedCentralPMCID:PMC3438318.

13:CookN,FreseKK,BapiroTE,JacobetzMA,GopinathanA,MillerJL,RaoSS,DemuthT,HowatWJ,JodrellDI,TuvesonDA.Gammasecretaseinhibitionpromoteshypoxicnecrosisinmousepancreaticductaladenocarcinoma.JExpMed.2012Mar12;209(3):437-44.doi:10.1084/jem.20111923.Epub2012Feb20.PubMedPMID:22351932;PubMedCentralPMCID:PMC3302221.

14:AsnaghiL,EbrahimiKB,SchreckKC,BarEE,CoonfieldML,BellWR,HandaJ,MerbsSL,HarbourJW,EberhartCG.Notchsignalingpromotesgrowthandinvasioninuvealmelanoma.ClinCancerRes.2012Feb1;18(3):654-65.doi:10.1158/1078-0432.CCR-11-1406.Epub2012Jan6.PubMedPMID:22228632.

15:Osanyingbemi-ObidiJ,DobromilskayaI,IlleiPB,HannCL,RudinCM.NotchsignalingcontributestolungcancerclonogeniccapacityinvitrobutmaybecircumventedintumOrigenesisinvivo.MolCancerRes.2011Dec;9(12):1746-54.doi:10.1158/1541-7786.MCR-11-0286.Epub2011Oct12.PubMedPMID:21994468;PubMedCentralPMCID:PMC3243765.

16:PandyaK,MeekeK,ClementzAG,RogowskiA,RobertsJ,MieleL,AlbainKS,OsipoC.TargetingbothNotchandErbB-2signallingpathwaysisrequiredforpreventionofErbB-2-positivebreasttumourrecurrence.BrJCancer.2011Sep6;105(6):796-806.doi:10.1038/bjc.2011.321.Epub2011Aug16.PubMedPMID:21847123;PubMedCentralPMCID:PMC3171020.

17:RamakrishnanV,AnsellS,HaugJ,GroteD,KimlingerT,StensonM,TimmM,WellikL,HallingT,RajkumarSV,KumarS.MRK003,aγ-secretaseinhibitorexhibitspromisinginvitropre-clinicalactivityinmultiplemyelomaandnon-Hodgkin'slymphoma.Leukemia.2012Feb;26(2):340-8.doi:10.1038/leu.2011.192.Epub2011Aug9.PubMedPMID:21826062.

18:LinH,XiongW,ZhangX,LiuB,ZhangW,ZhangY,ChengJ,HuangH.Notch-1activation-dependentp53restorationcontributestoresveratrol-inducedapoptosisinglioblastomacells.OncolRep.2011Oct;26(4):925-30.doi:10.3892/or.2011.1380.Epub2011Jul4.PubMedPMID:21743969.

19:ClementzAG,RogowskiA,PandyaK,MieleL,OsipoC.NOTCH-1andNOTCH-4arenovelgenetargetsofPEA3inbreastcancer:noveltherapeuticimplications.BreastCancerRes.2011Jun14;13(3):R63.doi:10.1186/bcr2900.PubMedPMID:21679465;PubMedCentralPMCID:PMC3218952.

20:CaoL,ZhouY,ZhaiB,LiaoJ,XuW,ZhangR,LiJ,ZhangY,ChenL,QianH,WuM,YinZ.Sphere-formingcellsubpopulationswithcancerstemcellpropertiesinhumanhepatomacelllines.BMCGastroenterol.2011Jun14;11:71.doi:10.1186/1471-230X-11-71.PubMedPMID:21669008;PubMedCentralPMCID:PMC3136412.

品牌介绍


MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务。

MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务和分子有竞争力的价格。MedKoo是您可靠的合作伙伴采购药物发现和药物分子。




苏州蚂蚁淘生物科技有限公司是一家创新型高科技生物公司,以常规生物学实验外包与生物学试剂为基础,放眼于生命科学领域的前沿技术服务,公司技术骨干有着多年的生物学科研背景,毕业于国内外名牌大学,并且有着丰富的项目经验,了解国内外科研行情,我公司力求为每一个客户提专业、针对性的实验方案。我公司以技术服务为支点,和国内外多家生物试剂公司有着密切的业务往来.公司特色技术服务包括:抗体药物研发、噬菌体抗体库、蛋白表达与传化、抗体制备、高通量测序、组学研究、生物信息学分析与方法建立、基础分子生物学技术外包、化学中间体合成、原料药物研发、论文编写等。我公司秉承”诚信做人,认真做事,服务至上“,希望用我们的专业知识和项目经验为国内科研客户解决科研问题,祝您科研之路畅通无阻!


CRISPR-Cas9 是近年兴起的用于靶向基因组特定位置,进行DNA修饰的重要工具。研究发现CRISPR是细菌为了应对病毒的攻击而演化而来的获得性免疫防御机制。具体来说,在CRISPR和Cas9的作用下,经由小RNA分子的引导,靶向并沉默入侵者遗传物质核酸的关键部分。在该系统中,crRNA(CRISPR-derived RNA)与tracrRNA(trans-activating RNA)结合形成的复合物能特异性识别靶基因序列,并引导Cas9核酸内切酶在靶定位点剪切双链DNA,随后,细胞的非同源末端连接修复机制(NHEJ)重新连接断裂处的基因组DNA,并引入插入或缺失突变。另外也可以提供一个外源双链供体DNA(Donor)通过同源重组(HR)整合进断裂处的基因组,从而达到对基因组DNA进行修饰的目的。
目前,CRISPR-Cas9系统的高效基因组编辑功能已被应用于多种生物,包括小鼠、大鼠、斑马鱼、秀丽隐杆线虫,也包含多种细菌和植物,甚至在人体上也有应用。
 
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