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当前位置: 首页 > 产品中心 > clinical_research > LKT/TOZASERTIB/T5996/25 mg
商品详细LKT/TOZASERTIB/T5996/25 mg
LKT/TOZASERTIB/T5996/25 mg
LKT/TOZASERTIB/T5996/25 mg
商品编号: T5996-25mg
品牌: lktlabs
市场价: ¥1540.00
美元价: 924.00
产地: 美国(厂家直采)
公司:
产品分类: 临床研究
公司分类: clinical_research
联系Q Q: 3392242852
电话号码: 4000-520-616
电子邮箱: info@ebiomall.com
商品介绍
  • Description
  • ProductInfo
  • ShippingandStorage
  • Downloads
  • References

Description

Tozasertibisananticancerchemotherapeuticpan-aurorakinase(AurK)inhibitorthatalsoinhibitsFMS-liketyrosinekinase3(FLT3)andAbl.Tozasertibiscurrentlyinclinicaltrialsasapotentialtreatmentforacutelymphoblasticleukemia(ALL).Incellularmodelsofcancer,tozasertibactivatescaspase-3andPARPanddecreasesexpressionofHDAC,increasingapoptosisandinhibitingcellgrowth.Inothercellularmodels,tozasertibinhibitscellproliferationandmetastasisbyblockingdownstreamERKsignalinganddownregulatingcdc25candcyclinB.Thiscompoundalsodecreasestumorgrowthinaninvivomodelofprostatecancer.

ProductInfo

CasNo.

639089-54-6

Purity

≥98%

Formula

C23H28N8OS

FormulaWt.

464.59

IUPACName

N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide

Synonym

VX680,MK0457

MeltingPoint

245-260°C

Solubility

DMSOat100mg/mL

Appearance

Whitetopaleyellowpowder

ShippingandStorage

StoreTemp

Ambient

ShipTemp

Ambient

Downloads

MSDS

T5996MSDSPDF

InfoSheet

T5996InfoSheetPDF

References

OkabeS,TauchiT,TanakaY,etal.ActivityofhistonedeacetylaseinhibitorsandanAurorakinaseinhibitorinBCR-ABL-expressingleukemiacells:CombinationofHDACandAurorainhibitorsinBCR-ABL-expressingcells.CancerCellInt.2013Apr4;13(1):32.PMID:23556431.

LiY,ZhouW,WeiL,etal.TheeffectofAurorakinasesoncellproliferation,cellcycleregulationandmetastasisinrenalcellcarcinoma.IntJOncol.2012Dec;41(6):2139-49.PMID:23007526.

GilesFJ,SwordsRT,NaglerA,etal.MK-0457,anAurorakinaseandBCR-ABLinhibitor,isactiveinpatientswithBCR-ABLT315Ileukemia.Leukemia.2013Jan;27(1):113-7.PMID:22772060.

JeetV,RussellPJ,VermaND,etal.Targetingaurorakinases:anovelapproachtocurbthegrowth&chemoresistanceofandrogenrefractoryprostatecancer.CurrCancerDrugTargets.2012Feb;12(2):144-63.PMID:22229247.

SalahE,UgochukwuE,BarrAJ,etal.CrystalstructuresofABL-relatedgene(ABL2)incomplexwithimatinib,tozasertib(VX-680),andatypeIinhibitorofthetriazolecarbothioamideclass.JMedChem.2011Apr14;54(7):2359-67.PMID:21417343.

OliveiraTM,AhmadR,EnghRA.VX680bindinginAuroraA:π-πinteractionsinvolvingtheconservedaromaticaminoacidoftheflexIBLeglycine-richloop.JPhysChemA.2011Apr28;115(16):3895-904.PMID:21306143.

品牌介绍
LKT Labs LKT Labs 是一家专注于防癌抗癌特殊化学品研究和开发的公司。主要提供:癌症药物、药物发现试剂盒、天然产物、广泛的生命科学研究试剂、定制合成。美国LKT Labs 是1988年在美国成立的,为全球提供先端的药物研发试剂、试剂盒、委托合成,并为药物生产企业提供原料,最近几年在农药、水产养殖业有很大程度的开发。在LKT Labs 可以找到在其他地方找不到的产品。 试剂