Cellagentech/PS-341(硼替佐米)|蛋白酶体抑制剂/C7734-5/5 mg(粉末)

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¥1780.00
货号:C7734-5
浏览量:127
品牌:Cellagen
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ProductDescription

Bortezomibisafirst-in-classdipeptideboronicacid-based,water-solubleproteasomeinhibitor.Asasingleagent,bortezomibwasfoundtohaveconsistentantitumoractivityinbothchemosensitiveandchemoresistantmultiplemyelomacellsatanIC50of10-20ng/mL.[1]BortezomibovercomestheresistancetoapoptosisinmultiplemyelomacellsthatisinducedbyIL-6.[2]Additionally,bortezomibpreventsTNF-a-induced,NF-kB-dependentupregulationofIL-6andreducescelladhesion;proliferationofremainingadherentmultiplemyelomacellswasalsoinhibitedbybortezomib.[1]

InMMcelllinesU266,IM-9,andHsSultan,bortezomibinhibitedatIC50concentrationsof3,6,and20nM,respectively.[2]CellgrowthofDox40,MR20,andLR5MMcellswascompletelyinhibitedbybortezomibat100nMIC50.

BortezomibsuppressesgrowthandinducesapoptosisinBcr/Abl-positivecellssensitiveandresistanttoIM.Interestingly,sequentialcombinationofbortezomibfollowedbyimatinibresultedinasynergisticpro-apoptoticeffectinimatinib-resistantcells;simultaneousexposureofbortezomibandimatinibwasantagoNISTic.[3]


Technicalinformation:

ChemicalFormula: C19H25BN4O4
CAS#: 179324-69-7
MolecularWeight: 384.24
Purity: >98%
Appearance: LightYellowCrystalline
ChemicalName: [(1R)-3-methyl-1-({(2S)-3-phenyl-2-[(pyrazin-2-ylcarbonyl)amino]propanoyl}amino)butyl]boronicacid
Solubility: Upto100mMinDMSO
Synonyms: PS-341,PS341,Bortezomib,Velcade,LDP-341

ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.


Reference:

1.Richardsonetal.,CancerControl,2003,10(6),361-369.
2.Hideshimaetal.,TheproteasomeinhibitorPS-341inhibitsgrowth,inducesapoptosis,andovercomesdrugresistanceinhumanmultiplemyelomacells.CancerRes.2001,61,3071-3076.PubmedID:1306489
3.Gattoetal.,TheproteasomeinhibitorPS-341inhibitsgrowthandinducesapoptosisinBcr/Abl-positivecelllinessensitiveandresistanttoimatinibmesylate.Haematologica,2003,88(8),853-863.PubmedID:12935973

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