Medchemexpress/LY2835219（同义词：ABEMACICLIB；CDK4/6双抑制剂）/HY-16297/10mg-免疫在线蚂蚁淘旗下平台

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商品详细Medchemexpress/LY2835219（同义词：ABEMACICLIB；CDK4/6双抑制剂）/HY-16297/10mg

Medchemexpress/LY2835219（同义词：ABEMACICLIB；CDK4/6双抑制剂）/HY-16297/10mg

商品编号： HY-16297-10mM*1mLinDMSO

品牌： MedChemExp

市场价： ¥1600.00

美元价： 960.00

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

LY2835219aselectiveCDK4/6inhibitorwithIC₅₀valuesof2nMand10nMforCDK4andCDK6,respectively.

CustomerValidation

•Nature.2017Aug24;548(7668):471-475.
•MolCell.2017Oct19;68(2):336-349.e6.
•NatCommun.2017Jun27;8:15916.
•CancerRes.2016Nov15;76(22):6723-6734.
•BiochimBiophysActa.2017Nov20;1865(2):354-363.
•MolOncol.2017Aug;11(8):1035-1049.

•Oncotarget.2017Jun27;8(40):67422-67438.
•BiochemPharmacol.2017Jan15;124:29-42.
•HarvardMedicalSchoolLINCSLIBRARY

Description	LY2835219aselectiveCDK4/6inhibitorwithIC₅₀valuesof2nMand10nMforCDK4andCDK6,respectively.
IC₅₀&Target	IC50:2nM(CDK4),10nM(CDK6)^[3]
InVitro	LY2835219reducescellviABIlitywiththeIC₅₀valuesrangingfrom0.5μMto0.7μM,inhibitsAktandERKsignalingbutnotmTORactivationatheadandnecksquamouscellcarcinoma(HNSCC)cells^[1].LY2835219showsinhibitiononA375R1-4,M14R,andSH4RwithEC₅₀valuesrangingfrom0.3to0.6μM;LY2835219inhibitstheproliferationoftheparentalA375andresistantA375RV1andA375RV2cellswithsimilarpotencieswithIC₅₀valuesof395,260,and463nM,respectively^[2].LY2835219inhibitsCDK4andCDK6withlownanomolarpotency,inhibitsRbphosphorylationresultinginaG1arrestandinhibitionofproliferation,anditsactivityisspecificforRb-proficientcells^[3].
InVivo	LY2835219(45mg/kg,p.o.)incombinationwitheverolimuscausesacooperativeantitumoreffectinHNSCCxenografttumor^[1].LY2835219(45or90mg/kg,p.o.)showssignificanttumorgrowthinhibitioninanA375xenograftmodel^[2].
References	[1].KuBM,etal.TheCDK4/6inhibitorLY2835219haspotentactivityincombinationwithmTORinhibitorinheadandnecksquamouscellcarcinoma.Oncotarget.2016Mar22;7(12):14803-13. [2].YadavV,etal.TheCDK4/6inhibitorLY2835219overcomesvemurafenibresistanceresultingfromMAPKreactivationandcyclinD1upregulation.MolCancerTher.2014Oct;13(10):2253-63. [3].GelbertLM,etal.PreclinicalcharacterizationoftheCDK4/6inhibitorLY2835219:in-vivocellcycle-dependent/independentanti-tumoractivitiesalone/incombinationwithgemcitabine.InvestNewDrugs.2014Oct;32(5):825-37. [4].WuT,etal.Effectofabemaciclib(LY2835219)onenhancementofchemotherapeuticagentsinABCB1andABCG2overexpressingcellsinvitroandinvivo.BiochemPharmacol.2017Jan15;124:29-42.

KinaseAssay ^[1]	Cells(5×10³)areplatedin96wellplates.Cellsaretreatedthenextdayfor24to48hoursandthenassessedforcaspase-3activitybyCaspase-Glo-3/7Assay,aspermanufacturer"sinstructionsandaluminescenceplatereader.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.
CellAssay ^[1]	LY2835219isdissolvedinDMSOtoa10mMconcentration. Cellsareseededina96-wellplate,allowedtoadhereovernight,andtreatedwithDMSOcontrol(0.1%v/v)ortheindicatedcompoundsfor72h.CellviabilityandproliferationaredeterminedusingaCellCountingKitaccordingtothemanufacturer"sinstructions.TheinteractionbetweenLY2835219andmTORinhibitorisdeterminedusingCompuSyn.Combinationindex(CI)valuesof1indicatesandadditivedruginteraction,whereasaCIof<1=""is=""synergistic=""and=""a=""ci=""of="">1isantagoNISTic.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.
AnimalAdministration ^[1]	LY2835219isdissolvedin1%HECin20mMphosphatebuffer. Six-week-oldBALB/cfemalenudemiceareinjectedsubcutaneouslywithOSC-19(1×10⁶)cells.Whentumorsizesreachapproximately100mm³,micearerandomizedbytumorsizeandsubjectedtoeachtreatment.Atleast5micepertreatmentgroupareincluded.Eachgroupofmiceisdosedviadailyoralgavagewithvehicle,LY2835219(45mg/kg/dor90mg/kg/d),Everolimus(5mg/kg/d),oracombinationofboth.TheLY2835219isdissolvedin1%HECin20mMphosphatebuffer(pH2.0).Tumorsizeandbodyweightaremeasuredtwiceweekly.Tumorvolumesarecalculatedusingthefollowingformula:V=(L×W²)/2(L,Length;W,width).Micearegavagedafinaltimeonday14andsacrificedthefollowingday.ThetumorsareremovedforWesternblotandimmunohistochemistry.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.
References	[1].KuBM,etal.TheCDK4/6inhibitorLY2835219haspotentactivityincombinationwithmTORinhibitorinheadandnecksquamouscellcarcinoma.Oncotarget.2016Mar22;7(12):14803-13. [2].YadavV,etal.TheCDK4/6inhibitorLY2835219overcomesvemurafenibresistanceresultingfromMAPKreactivationandcyclinD1upregulation.MolCancerTher.2014Oct;13(10):2253-63. [3].GelbertLM,etal.PreclinicalcharacterizationoftheCDK4/6inhibitorLY2835219:in-vivocellcycle-dependent/independentanti-tumoractivitiesalone/incombinationwithgemcitabine.InvestNewDrugs.2014Oct;32(5):825-37. [4].WuT,etal.Effectofabemaciclib(LY2835219)onenhancementofchemotherapeuticagentsinABCB1andABCG2overexpressingcellsinvitroandinvivo.BiochemPharmacol.2017Jan15;124:29-42.

MolecularWeight

602.7

Formula

C₂₈H₃₆F₂N₈O₃S

CASNo.

1231930-82-7

Storage

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

Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

H₂O:≥250mg/mL

LY2835219isdissolvedin1%HECin20mMphosphatebuffer(pH2.0)andadministeredorallybygavage(finalvolume0.2mL)^[4].

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

References

[1].KuBM,etal.TheCDK4/6inhibitorLY2835219haspotentactivityincombinationwithmTORinhibitorinheadandnecksquamouscellcarcinoma.Oncotarget.2016Mar22;7(12):14803-13.
[2].YadavV,etal.TheCDK4/6inhibitorLY2835219overcomesvemurafenibresistanceresultingfromMAPKreactivationandcyclinD1upregulation.MolCancerTher.2014Oct;13(10):2253-63.
[3].GelbertLM,etal.PreclinicalcharacterizationoftheCDK4/6inhibitorLY2835219:in-vivocellcycle-dependent/independentanti-tumoractivitiesalone/incombinationwithgemcitabine.InvestNewDrugs.2014Oct;32(5):825-37.
[4].WuT,etal.Effectofabemaciclib(LY2835219)onenhancementofchemotherapeuticagentsinABCB1andABCG2overexpressingcellsinvitroandinvivo.BiochemPharmacol.2017Jan15;124:29-42.

Purity:99.87%

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