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蚂蚁淘在线 / 品牌中心 / MCE / Medchemexpress/Verteporfin(Synonyms: CL 318952)/HY-B0146/10mM*1mL in DMSO

Medchemexpress/Verteporfin(Synonyms: CL 318952)/HY-B0146/10mM*1mL in DMSO

价格
￥3040.00
货号：HY-B0146-10mM*1mLinDMSO
浏览量：127
品牌：MCE
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商品描述
VerteporfinisabenzoporphyrinderivativemonoacidringA,andcaninhibittheactivityofYAP.
Description

VerteporfinisabenzoporphyrinderivativemonoacidringA,andcaninhibittheactivityofYAP.

InVitro

VerteporfinisspecificallyselectedbyPDX-cellscreening.Theconcentrationstocause50%growthinhibition(GI50)forPhLO,PhLH,andPhLKare228nM,395nM,and538nM,respectively,whereasGI50forALL-1,TCC-Y/sr,andNPhA1are3.93µM,2.11µM,and5.61µM,respectively.GSHsignificantlyreducesthesensitivityof2outof3PDXcellstoverteporfin.VerteporfinreducesthemitochondrialmembranepotentialinPDXcells[1].VerteporfinreducesthePTX-resistanceonHCT-8/TcellsbyinhibitingYAPexpressionandcombinationtherapywithverteporfinandpaclitaxel(PTX)showssynergismoninhibitionofYAPandcytotoxicitytoHCT-8/T[2].

InVivo

Verteporfin(10mg/kg,c.s.c.)anddasatinibsignificantlyreducestheleukemiacellratio,andcombinedtherapyfurtherreducedthenumberofleukemiacellsinthespleen[1].

ClinicalTrial
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References

  • [1].MorishitaT,etal.Thephotosensitizerverteporfinhaslight-independentanti-leukemicactivityforPh-positiveacutelymphoblasticleukemiaandsynergisticallyworkswithdasatinib.Oncotarget.2016Aug2.

    [2].PanW,etal.VerteporfincanReversethePaclitaxelResistanceInducedbyYAPOver-ExpressioninHCT-8/TCellswithoutPhotoactivationthroughInhibitingYAPExpression.CellPhysiolBiochem.2016;39(2):481-90.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.3912mL6.9561mL13.9123mL
5mM0.2782mL1.3912mL2.7825mL
10mM0.1391mL0.6956mL1.3912mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[1]

VerteporfinisdissolvedinDMSO.

PDXcellsco-culturedwithS17cellsaretreatedwith16combinationsofverteporfin(60nM,120nM,180nM,and240nM)anddasatinib(12nM,24nM,36nM,and48nM).TheviABIlitiesofcellstreatedwitheachcombinationaremeasuredafter48husingFACSAriaflowcytometer.Inordertoestimatedruginteractionbetweenverteporfinanddasatinib,anormalizedisobologramandfractionaffectedcombinationindex(CI)plotaremadeusingCompuSynsoftware.CIvaluesgreaterthan1.0indicatedantagoNISTiceffects,equalto1.0additiveeffects,andbelow1.0synergisticeffects.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[1]

PhLOcells(1.0×107/mouse)areinjectedintravenouslyinto6-week-oldmaleNOGmice,whicharethentreatedwithvehicle,verteporfin(140mg/kg/day),dasatinib(20mg/kg/day),andacombinationofthesedrugsfromdays22to28.Verteporfinisadministeredbycontinuoussubcutaneousinfusion(c.s.c.)usingAlzetosmoticpumps.Anintraperitonealinjection(i.p.)isperformedfordasatinib.Allmicearesacrificedonday28andthechimerismofleukemiacellsisinvestigatedbyflowcytometerusingananti-humanCD19antibodyandantimouseCD45antibody.BloodconcentrationsofverteporfinarecalculatedbyLCMS-2020.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].MorishitaT,etal.Thephotosensitizerverteporfinhaslight-independentanti-leukemicactivityforPh-positiveacutelymphoblasticleukemiaandsynergisticallyworkswithdasatinib.Oncotarget.2016Aug2.

    [2].PanW,etal.VerteporfincanReversethePaclitaxelResistanceInducedbyYAPOver-ExpressioninHCT-8/TCellswithoutPhotoactivationthroughInhibitingYAPExpression.CellPhysiolBiochem.2016;39(2):481-90.

MolecularWeight

718.79

Formula

C₄₁H₄₂N₄O₈

CASNo.

129497-78-5

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:5.6mg/mL

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

Purity:99.26%