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Bpsbioscience/IPI504 (Retaspimycin hydrochloride)/277531/10 mg
MW:624.2Da
CASRegistry#:857402-63-2
Formula:C31H46ClN3O8
Target:HSP90
Background:
CancercellsdependontheHsp90chaperonetomaintainmanyproteinscriticalforcancergrowth,proliferationandsurvivalinafunctionalstate.RetaspimycinbindstoandinhibitsthecytosolicchaperonefunctionsofHSP90,whichmaintainsthestabilityandfunctionalshapeofmanyoncogenicsignalingproteinsandmaybeoverexpressedoroveractiveintumorcells.Retaspimycin-mediatedinhibitionofHSP90promotestheproteasomaldegradationofoncogenicsignalingproteinsinsusceptibletumorcellpopulations,whichresultsintheinductionofapoptosis.
Description:
Retaspimycinhydrochloride(alsoknownasIPI-504),ahydroquinonehydrochloridesaltderivativeof17-AAG,isanovel,potentandselectiveinhibitorofHsp90thatbindsattheN-terminalATP/ADP-bindingsiteofHsp90.Onceinthesystemiccirculation,IPI-504isdeprotonatedandconvertedintothefreebaseIPI-504whichissubsequentlyoxidizedto17-AAG.
Synonym(s):
IPI-504;Retaspimycinhydrochloride;
BiologicalActivity:
IPI-504potentlyinhibitsproliferationinseveraltumorcelllineswith50%inhibitionconcentrationIC50valuesrangingfrom10-40nMandhasbeenusedforthetreatmentofgastrointestinalstromaltumors,soft-tissuesarcomasandnon-smallcelllungcancer.
Solubility:
SolubleinDMSO
Storage/Stability:

Storeatorbelow–20°C.Solidformisstableatleast12monthsfromdateofreceipt,whenstoredasdirected.Donotstoreaqueoussolutionsformorethanoneday.

Reference(s):
1.Siegel,D.,etal.Leukemia&Lymphoma,2011;52(12):2308-2315.
2.Leow,CC.,etal.MolCancerTher2009;8:2131-2141.
ScientificCategory:
HSPInhibitor
ProductType:
Inhibitor
Datashownislot-specific.Contactusforspecificinformationonotherlots.

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