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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