Medchemexpress/Ruxolitinib磷酸盐（同义词：INCB018424磷酸盐；INCB 018424磷酸盐；INCB-018424磷酸盐；鲁克索利蒂尼-免疫在线蚂蚁淘旗下平台

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商品详细Medchemexpress/Ruxolitinib磷酸盐（同义词：INCB018424磷酸盐；INCB 018424磷酸盐；INCB-018424磷酸盐；鲁克索利蒂尼

Medchemexpress/Ruxolitinib磷酸盐（同义词：INCB018424磷酸盐；INCB 018424磷酸盐；INCB-018424磷酸盐；鲁克索利蒂尼

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

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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

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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

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	2.4730mL	12.3652mL	24.7304mL
5mM	0.4946mL	2.4730mL	4.9461mL
10mM	0.2473mL	1.2365mL	2.4730mL

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°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

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%

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