DasatinibisananticancerchemotherapeuticcompoundthatinhibitsAbl,PDGFR,ephrinreceptors,Src,c-Kit,andotherSrc-familykinases(LCK,HCK,FYN,andothers).Dasatinibisclinicallyusedtotreatchronicmyelogenousleukemia(CML)andacutelymphocyticleukemia(ALL);inacutemyelogenousleukemia(AML)cells,dasatinibinducesmyeloiddifferentiationandautophagy.Dasatinibalsodisplaysantiviralactivity,preventingdenguevirusinfectionthroughitsinhibitionofFYNkinase.
| CasNo. | 863127-77-9 |
|---|---|
| Purity | ≥98% |
| Formula | C22H26ClN7O2S•H2O |
| FormulaWt. | 506.02 |
| ChemicalName | N-(2-chlro-6-methylphenyl)-2-[[6-[4[(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamidemonohydrate |
| IUPACName | N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide;hydrate |
| MeltingPoint | 280-286°C |
| Solubility | Sparinglysolubleinwater(5.06mg/ml),andethanol.SolubleinDMSO(200mg/ml). |
| Appearance | WhitetoPaleYellowCrystalPowder |
| StoreTemp | Ambient |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | D0375InfoSheetPDF |
|---|
XieN,ZhongL,LiuL,etal.Autophagycontributestodasatinib-inducedmyeloiddifferentiationofhumanacutemyeloidleukemiacells.BiochemPharmacol.2014May1;89(1):74-85.PMID:24607273.
deWispelaereM,LaCroixAJ,YangPL.ThesmallmoleculesAZD0530anddasatinibinhibitdenguevirusRNAreplicationviaFynkinase.JVirol.2013Jul;87(13):7367-81.PMID:23616652.
MonteroJC,SeoaneS,OcañaA,etal.InhibitionofSRCfamilykinasesandreceptortyrosinekinasesbydasatinib:possIBLecombinationsinsolidtumors.ClinCancerRes.2011Sep1;17(17):5546-52.PMID:21670084.
DasJ,ChenP,NorrisD,etal.2-aminothiazoleasanovelkinaseinhibitortemplate.Structure-activityrelationshipstudiestowardthediscoveryofN-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide(dasatinib,BMS-354825)asapotentpan-Srckinaseinhibitor.JMedChem.2006Nov16;49(23):6819-32.PMID:17154512.
