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商品描述
MW:574.7Da
CASRegistry#:819812-04-9
Formula:C30H42N2O9
Target:HSP90
Background:
Heatshockprotein90(Hsp90)isapromisingtargetforanti-tumortherapy.KW-2478enhancedbortezomib-inducedcellgrowthinhibition,andexhibitedenhancedanti-tumoractivityagainsthumanmyeloma.
Description:
KW-2478isanovelandpotentnonansamycininhibitorofheatshockprotein90(IC50=3.8nM)designedtoovercomethelimitations,includinglowwatersolubilityandhepatotoxicity,of17-allylamino-17-demethoxygeldanamycin(17-AAG).KW-2478exertsastrongantitumoractivityagainstmultiplemyeloma(MM)cellswithvariouschromosormaltranslocations.KW-2478inhibitscellgrowthandapoptosisassociatedwithHsp90clientproteindegradation.RecentstudyresultshaverevealedthatKW-2478isabletodepleteHsp90clientCdk9andthephosphorylated4E-BP1,atranscriptionalkinaseandatranscriptioninhibitorrespectively,leADIngtoreducedexpressionofFGFR3,c-MafandcyclinD1.
Synonym(s):
KW2478;KW2478
Solubility:
SolubleinDMSO
Storage/StABIlity:
Storeatorbelow–20°C.Solidformisstableatleast12monthsfromdateofreceipt,whenstoredasdirected.Donotstoreaqueoussolutionsformorethanoneday.
Reference(s):
1.NakashimaT,etal.ClinCancerRes.2010;16(10):2792-802.
2.Ishii,T.,etal.BloodCancerJ.2012Apr;2(4):e68.
2.Ishii,T.,etal.BloodCancerJ.2012Apr;2(4):e68.
ScientificCategory:
HSPInhibitor
ProductType:
Inhibitor
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