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Tocris/GSK 1838705/5111/50/50 mg
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Tocris/GSK 1838705/5111/50/50 mg
品牌 / 
Tocris
货号 / 
5111/50
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4000-520-616
Description:PotentIRandIGF1Rinhibitor;alsoinhibitsanaplasticlymphomakinase(ALK)
ChemicalName:2-[[2-[[1-[(Dimethylamino)ethanoyl]-5-(methyloxy)-2,3-dihydro-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide
Purity:≥98%(HPLC)
BIOLOGicalActivityTechnicalDataSolubilityCalculatorsDatasheetsReferences

BiologicalActivity

Potentinsulinreceptor(IR)andinsulin-likegrowthfactor-1receptor(IGF1R)inhibitor(IC50valuesare1.6and2nM,respectively).Alsoinhibitsanaplasticlymphomakinase(ALK)(IC50=0.5nM).Displays>800-foldselectivityforIR,IGFR1andALKoverapanelof44kinasesincludingJNK.Blocksproliferationofcancercelllinesinvitro,andcausescompleteregressionofALK-dependenttumorsinvivo.Orallybioavailable.

LicensingInformation

SoldforresearchpurposesunderagreementfromGlaxoSmithKline.

CompoundLibraries

GSK1838705isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.

TechnicalData

M.Wt532.57
FormulaC27H29FN8O3
StorageStoreat-20°C
Purity≥98%(HPLC)
CASNumber1116235-97-2
PubChemID25182616
InChIKeyHZTYDQRUAWIZRE-UHFFFAOYSA-N
SmilesO=C(CN(C)C)N4CCC(C4=C5)=CC(OC)=C5NC1=NC(NC3=C(C(NC)=O)C(F)=CC=C3)=C2C(NC=C2)=N1

Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.

AllTocrisproductsareintendedforlaboratoryresearchuseonly.

SolubilityData

SolventMaxConc.mg/mLMaxConc.mM
Solubility
DMSO53.26100

PreparingStockSolutions

Thefollowingdataisbasedontheproductmolecularweight532.57.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.

Concentration/SolventVolume/Mass1mg5mg10mg
1mM1.88mL9.39mL18.78mL
5mM0.38mL1.88mL3.76mL
10mM0.19mL0.94mL1.88mL
50mM0.04mL0.19mL0.38mL

ProductDatasheets

CertificateofAnalysis/ProductDatasheet
SafetyDatasheet