Bpsbioscience/NVP-BEP800/27766-1/10毫克
商品编号：
27766-1
品牌：
bpsbioscience
市场价：
¥5200.00
美元价：
3120.00
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
MW:480.4Da
CASRegistry#:847559-80-2
Formula:C21H23Cl2N5O2S
Target:Hsp90β
Background:
NVP-BEP800bindstotheN-terminalATP-bindingpocketofHsp90.Hsp90isaubiquitouslyexpressedmolecularchaperonewithATPaseactivityinvolvedintheconformationalmaturationandstABIlityofkeysignalingmoleculesinvolvedincellproliferation,survival,andtransformation.InBT-474cellsandA375cells,NVP-BEP800causestheHsp90-p23dissociationandclientproteindegradation(ErbB2)aswellasthereductionofclientproteinphosphorylation(phospho-Akt).Degradationoftheseoncogenicclientproteinsresultsintumorcellgrowtharrestanddeath.
Description:
NVP-BEP800isanovel,fullysynthetic,orallybioavailableinhibitorthatbindstotheNH(2)-terminalATP-bindingpocketofHsp90.NVP-BEP800(alsoknownasVER-82576)isanovelATP-competitiveHSP90βinhibitorthatbindstotheNH(2)-terminalATP-bindingpocketofHeatshockprotein90(Hsp90).NVP-BEP800inducedrobustantitumorresponsesintumorxenograftmodels,includingregressionintheBT-474breastcancermodel.NVP-BEP800canrADIosensitisetumourcelllinesofdifferententitiesthroughdestabilisationanddepletionofseveralHsp90clientproteins,thuscausingthedepletionofSphaseandG2/Marrest,increasedDNAdamageandrepairprotractionand,tosomeextent,apoptosis.
Synonym(s):
VER-82576;2-amino-4-[2,4-dichloro-5-(2-pyrrolidin-1-ylethoxy)phenyl]-N-ethylthieno[2,3-d]pyrimidine-6-carboxamide
BIOLOGicalActivity:
NVP-BEP800isanATP-competitiveinhibitorofHsp90β,withanIC50of58nMinacompetitivebindingfluorescencepolarizationassay.Exhibits>70-foldselectivityagainstHsp90familymembersGrp94andTrap-1withIC50valuesof4.1µMand5.5µM,respectively.NVP-BEP800displaysnoinhibitoryactivityagainstthecloselyrelatedGHKLATPase,topoisomeraseII,andthestructurallyunrelatedATPase,Hsp70attheconcentrationof10µM.NVP-BEP800potentlyinhibitstheproliferationofvarioustumorcelllineswithGI50valuesrangingfrom38nMinA375to1.05µMinPC3(averageGI50of245nM),and46primaryhumantumors,includingsmallcelllung,mammarycancerandmelanoma,withthemeanIC50of0.75µMandIC70of1.8µM.Didnotinhibit20differentproteinkinasesatIC50>10µM.averageGI50of245nM.Additionally,treatmentofNVP-BEP800inducesapoptosisinhumanbreastcancercelllines.TheantitumorefficacyofNVP-BEP800isalsoobservedwithadoseof15or30mg/kg/dinA375xenograft-bearingmiceaswellasinBT-474breastcancerxenografts.
Solubility:
SolubleinDMSO
Storage/Stability:
Storeatorbelow–20°C.Solidformisstableatleast12monthsfromdateofreceipt,whenstoredasdirected.Donotstoreaqueoussolutionsformorethanoneday.
Reference(s):
MasseyAJ,etal.MolCancerTher.2010Apr;9(4):906-19.
ScientificCategory:
HSPInhibitor
ProductType:
Inhibitor
Datashownislot-specific.Contactusforspecificinformationonotherlots.
品牌介绍
bpsbioscience简介：为生命科学研究提供ELISA试剂盒（仅供科研）、抗体和抗原（仅供科研）、流式抗体，使您的检测结果更稳定可靠，用心服务科研。我公司国内总代理,华东地区代理bpsbioscience 专业经营进口胎牛血清、细胞因子、ELISA试剂盒、细胞、抗体、生物试剂、耗材、培养基、一抗、二抗、其产品吸附均匀，吸附性好，空白值低，孔底透明度高，代做ELISA实验等。
