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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/硼替佐米（同义词：PS-341）/HY-10227/10mM*1mL二甲基亚砜
商品详细Medchemexpress/硼替佐米（同义词：PS-341）/HY-10227/10mM*1mL二甲基亚砜
Medchemexpress/硼替佐米（同义词：PS-341）/HY-10227/10mM*1mL二甲基亚砜
Medchemexpress/硼替佐米（同义词：PS-341）/HY-10227/10mM*1mL二甲基亚砜
商品编号： HY-10227-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1320.00
美元价： 792.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
电子邮箱： info@ebiomall.com
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商品介绍
Bortezomibisapotent20SproteasomeinhibitorwithKiof0.6nM.

CustomerValidation

  • •NatCommun.2017May22;8:15398.
  • •StemCellReports.2017Nov23.pii:S2213-6711(17)30483-6.
  • •EurJPharmacol.2017Nov15;815:147-155.
  • •BiochemBiophysResCommun.2016May13;473(4):1125-32.
  • •Patent.US20160222465A1.
  • •HarvardMedicalSchoolLINCSLIBRARY
Description

Bortezomibisapotent20SproteasomeinhibitorwithKiof0.6nM.

IC50&Target

Ki:0.6nM(20Sproteasome)[1]

InVitro

Bortezomib(PS-341)effectsproteinsthatcontrolcellcycleprogression.TreatmentofPC-3cellswithBortezomib(100nM)for8hresultsintheaccumulationofcellsinG2-M,withacorrespondingdecreaseinthenumberofcellsinG1.TheBortezomibdosesatwhich50%ofPC-3cellsarekilledat24and48haredeterminedtobe100and20nM,respectively[1].Bortezomibisahighlyselective,reversIBLeinhibitorofthe26Sproteasome.InhibitionoftheproteasomebyBortezomibresultsinactivationofJNK,stABIlizationofp53,Bid,Bax,p21,p27,caveolin-1,andIκBα,resultingininhibitionofNF-κB[2].TheIC50ofBortezomibisfoundtobe2.46nMfor26SproteasomeintheB16F10cells[3].

InVivo

MicebearingPC-3tumorsaretreatedwithBortezomib(i.v.,0.3or1.0mg/kg).Bortezomib(1.0mg/kg)resultsinasignificantdecreaseintumorgrowth~60%.Bortezomib(0.3mg/kg)producesa16%decreaseintumorvolumebutdidnotreachsignificance[1].Bortezomib(0.2mg/kg)significantlydecreasesthewithdrawalthresholdondays11and15andincreasesthenumberofwithdrawalresponsesondays11and15comparedwiththevehiclegroupinthevonFreyandacetonetests[4].

ClinicalTrial
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References

  • [1].AdamsJ,etal.Proteasomeinhibitors:anovelclassofpotentandeffectiveantitumoragents.CancerRes.1999Jun1;59(11):2615-22.

    [2].BoccadoroM,etal.Preclinicalevaluationoftheproteasomeinhibitorbortezomibincancertherapy.CancerCellInt.2005Jun1;5(1):18.

    [3].YerlikayaA,etal.CombinedeffectsoftheproteasomeinhibitorbortezomibandHsp70inhibitorsontheB16F10melanomacellline.MolMedRep.2010Mar-Apr;3(2):333-9.

    [4].YamamotoS,etal.Behavioralandpharmacologicalcharacteristicsofbortezomib-inducedperipheralneuropathyinrats.JPharmacolSci.2015Sep;129(1):43-50.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.6025mL13.0127mL26.0254mL
5mM0.5205mL2.6025mL5.2051mL
10mM0.2603mL1.3013mL2.6025mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[1]

BortezomibisdissolvedinDMSOandstored,andthendilutedwithappropriatemedia(DMSO0.1%)beforeuse[1].

ThehumanPC-3prostatetumorcellsaretreatedwithBortezomib(0.1nM,1nM,10nM,100nM,1μM,10μM)for24-48hincompletemedium.CytotoxicityismeasuredusingaMTTassay[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[1][4]

Bortezomibispreparedin98%saline(0.9%),2%ethanol,and0.1%ascorbicacid(Mice)[1].
Bortezomibisdissolvedin5%DMSOsolution(Rat)[4].

Mice[1]
Malenudemice(18-20g;n=51)areused.Bortezomib(0.3or1.0mg/kg)isadministeredinvehiclei.v.usingadosevolumeof100μLpermouseordirectlyintothetumorina10μLvolume.DuetothecomparativelyhighlevelsofBortezomibintheprostate,afteri.v.dosingofradiolabeleddrug,itisdecidedtoexaminetheeffectsofthisnovelcompoundintheprostate,PC-3,xenografttumormodel.Animalsaretreatedwhenthetumorsbecomepalpable(>300mm3).Malenudemice(18-20g;n=51)areused.Bortezomib(0.3or1.0mg/kg)isadministeredinvehiclei.v.usingadosevolumeof100μLpermouseordirectlyintothetumorina10μLvolume.DuetothecomparativelyhighlevelsofBortezomibintheprostate,afteri.v.dosingofradiolabeleddrug,itisdecidedtoexaminetheeffectsofthisnovelcompoundintheprostate,PC-3,xenografttumormodel.Animalsaretreatedwhenthetumorsbecomepalpable(>300mm3).
Rat[4]
MaleSprague-Dawleyratsweighing200-250gareused.Bortezomib(0.05,0.1,or0.2mg/kg)orvehicle(5%DMSOsolution)isadministeredintraperitoneally(i.p.)twiceaweekfor2weeks(ondays1,4,8,and11).TheadministrationscheduleanddosesofBortezomibaredeterminedbasedonclinicaltreatment(1.3mg/m2ofBortezomibondays1,4,8,and11).MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].AdamsJ,etal.Proteasomeinhibitors:anovelclassofpotentandeffectiveantitumoragents.CancerRes.1999Jun1;59(11):2615-22.

    [2].BoccadoroM,etal.Preclinicalevaluationoftheproteasomeinhibitorbortezomibincancertherapy.CancerCellInt.2005Jun1;5(1):18.

    [3].YerlikayaA,etal.CombinedeffectsoftheproteasomeinhibitorbortezomibandHsp70inhibitorsontheB16F10melanomacellline.MolMedRep.2010Mar-Apr;3(2):333-9.

    [4].YamamotoS,etal.Behavioralandpharmacologicalcharacteristicsofbortezomib-inducedperipheralneuropathyinrats.JPharmacolSci.2015Sep;129(1):43-50.

MolecularWeight

384.24

Formula

C₁₉H₂₅BN₄O₄

CASNo.

179324-69-7

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

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

Purity:99.71%