ProductDescription
TG101348isanorally-available,aminopyrimidine-basedinhibitorofJAK2andJAK2V617FatanIC50of3nM,withmarkedselectivityoverJAK3(IC50>1uM).[1,2]TG101348inhibitsproliferationofHMC-1.1andHMC-1.2cellsatIC50sof740and407nM,respectively.[1]
InaUT7/EPOcellline,TG101348inhibitedSTAT5phosphorylationmuchmorepotentlyatlowerconcentrationsthanknownJAK2/3inhibitorAG490(600nMvs100uM).Inthesamestudy,TG101348inhibitedAKTphosphorylationwhilereducingGATA-1S310phosphorylation.[2]
InhumanerythroleukemiaandBa/F3-JAK2V617Fcells,TG101348inhibitedthecytokine-independentgrowthatIC50sof300and580nM,respectively.[3]
TG101348inducesapoptosisinbothHELandBa/F3JAK2V617Fcells,butnotinnormalhumandermalfibroblastsatconcentrationsupto10uM;antiproliferativeIC50againstfibroblastsis>5uM.
Technicalinformation:
| ChemicalFormula: | C27H36N6O3S | |
| CAS#: | 936091-26-8 | |
| MolecularWeight: | 524.68 | |
| Purity: | >98% | |
| Appearance: | PaleYellow | |
| ChemicalName: | N-tert-butyl-3-(5-methyl-2-(4-(2-(pyrrolidin-1-yl)ethoxy)phenylamino)pyrimidin-4-ylamino)benzenesulfonamide | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | TG101348,TG-101348,SAR302503 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Lashoetal.,InhibitionofJAK-STATsignalingbyTG101348:anovelmechanismforinhibitionofKITD816V-dependentgrowthinmastcellleukemiacells.Leukemia,2010,24,1378-1380.PubmedID:20485374 |
| 2. | Geronetal.,SelectiveinhibitionofJAK2-drivenerythroiddifferentiationofpolycythemiaveraProgenitors.CancerCell,2008,13(4),321-330.PubmedID:18394555 |
| 3. | Lashoetal.,TG101348,aJAK2-selectiveantagoNIST,inhibitsprimaryhematopoieticcellsderivedfrommyeloproliferativedisorderpatientswithJAK2V617F,MPLW515KorJAK2exon12mutationsaswellasmutationnegativepatients.Leukemia,2008,22,1790-1792.PubmedID:18354492 |
| 4. | Wernigetal.,EfficacyofTG101348,aselectiveJAK2inhibitor,intreatmentofamurinemodelofJAK2V617F-inducedpolycythemiavera.CancerCell2008,13(4),311-320.PubmedID:18394555 |
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