4000-520-616
欢迎来到免疫在线！(蚂蚁淘生物旗下平台)  请登录 |  免费注册 |  询价篮
产品库 品牌馆 现货促销 技术交流 新闻动态 联系我们
MedChemExp
主营：主营：抑制剂、激动剂、API
咨询热线电话
4000-520-616
公司首页 公司介绍 产品中心 新闻动态 联系方式 在线下单
当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Ruxolitinib phosphate（同义词：INCB018424 phosphate；INCB 018424磷酸盐；INCB-018424磷酸盐；鲁索里蒂尼
商品详细Medchemexpress/Ruxolitinib phosphate（同义词：INCB018424 phosphate；INCB 018424磷酸盐；INCB-018424磷酸盐；鲁索里蒂尼
Medchemexpress/Ruxolitinib phosphate（同义词：INCB018424 phosphate；INCB 018424磷酸盐；INCB-018424磷酸盐；鲁索里蒂尼
Medchemexpress/Ruxolitinib phosphate（同义词：INCB018424 phosphate；INCB 018424磷酸盐；INCB-018424磷酸盐；鲁索里蒂尼
商品编号： HY-50858-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1320.00
美元价： 792.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
电子邮箱： info@ebiomall.com
立即询价
商品介绍
Ruxolitinib(phosphate)isthefirstpotentJAK1/2inhibitorwithIC50valuesof3.3nM/2.8nM,morethan130-foldselectivityforJAK1/2versusJAK3.

CustomerValidation

  • •Blood.2013Nov21;122(22):3628-31.
  • •InflammRes.2015Jan;64(1):41-51.
  • •HarvardMedicalSchoolLINCSLIBRARY
Description

Ruxolitinib(phosphate)isthefirstpotentJAK1/2inhibitorwithIC50valuesof3.3nM/2.8nM,morethan130-foldselectivityforJAK1/2versusJAK3.

IC50&Target

IC50:3.3nM(JAK1),2.8nM(JAK2)

InVitro

Ruxolitinib(INCB018424)potentlyandselectivelyinhibitsJAK2V617F-mediatedsignalingandproliferation.RuxolitinibinhibitsthegrowthofHELcellswithEC50of186nM.RuxolitinibmarkedlyincreasesapoptosisinBa/F3-EpoR-JAK2V617Fcellsystem,andinhibitshematopoieticProgenitorcellproliferationinprimaryMPNpatientsamples[1].

InVivo

Ruxolitinib(180mg/kg,p.o.)reducesthetumorburdenofmiceinoculatedwithJAK2V617F-expressingcellswithoutcausinganemiaorlymphopenia[1].

ClinicalTrial
ViewMoreCollapse
References

  • [1].Quintas-CardamaA,etal.PreclinicalcharacterizationoftheselectiveJAK1/2inhibitorINCB018424:therapeuticimplicationsforthetreatmentofmyeloproliferativeneoplasms.Blood,2010,115(15),3109-3117.

    [2].FleischmanAG,etal.TheCSF3RT618ImutationcausesalethalneutrophilicneoplasiainmicethatisresponsivetotherapeuticJAKinhibition.Blood.2013Nov21;122(22):3628-31.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.4730mL12.3652mL24.7304mL
5mM0.4946mL2.4730mL4.9461mL
10mM0.2473mL1.2365mL2.4730mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[1]

Ruxolitinibphosphateisdissolvedin0.2%DMSO.

Cellsareseededat2000/wellofwhitebottom96-wellplates,treatedwithcompoundsfromDMSOstocks(0.2%finalDMSOconcentration),andincubatedfor48hoursat37°Cwith5%CO2.ViABIlityismeasuredbycellularATPdeterminationusingtheCell-TiterGloluciferasereagentorviablecellcounting.Valuesaretransformedtopercentinhibitionrelativetovehiclecontrol,andIC50 curvesarefittedaccordingtononlinearregressionanalysisofthedatausingPRISMGraphPad.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[1]

Ruxolitinibphosphateisdissolvedinvehicle(5%dimethylacetamide,0.5%methocellulose).

Micearefedstandardrodentchowandprovidedwithwateradlibitum.Ba/F3-JAK2V617Fcells(105 permouse)areinoculatedintravenouslyinto6-to8-week-oldfemaleBALB/cmice.Survivalismonitoreddaily,andmoribundmicearehumanelykilledandconsidereddeceasedattimeofdeath.Treatmentwithvehicle(5%dimethylacetamide,0.5%methocellulose)orRuxolitinib(INCB018424)beginswithin24hoursofcellinoculation,twicedailybyoralgavage.HematologicparametersaremeasuredusingaBayerAdvia120analyzed,andstatisticalsignificanceisdeterminedusingDunnetttesting.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].Quintas-CardamaA,etal.PreclinicalcharacterizationoftheselectiveJAK1/2inhibitorINCB018424:therapeuticimplicationsforthetreatmentofmyeloproliferativeneoplasms.Blood,2010,115(15),3109-3117.

    [2].FleischmanAG,etal.TheCSF3RT618ImutationcausesalethalneutrophilicneoplasiainmicethatisresponsivetotherapeuticJAKinhibition.Blood.2013Nov21;122(22):3628-31.

MolecularWeight

404.36

Formula

C₁₇H₂₁N₆O₄P

CASNo.

1092939-17-7

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥31mg/mL;H2O:5.4mg/mL(Needultrasonicorwarming)

Ruxolitinibphosphateisdissolvedin5%dimethylacetamide,0.5%methylcellulose[2].

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

References

  • [1].Quintas-CardamaA,etal.PreclinicalcharacterizationoftheselectiveJAK1/2inhibitorINCB018424:therapeuticimplicationsforthetreatmentofmyeloproliferativeneoplasms.Blood,2010,115(15),3109-3117.

    [2].FleischmanAG,etal.TheCSF3RT618ImutationcausesalethalneutrophilicneoplasiainmicethatisresponsivetotherapeuticJAKinhibition.Blood.2013Nov21;122(22):3628-31.

Purity:99.89%