BiologicalActivity
Dualinhibitoroftheinsulinreceptor(IR)andinsulin-likegrowthfactor-1receptor(IGF1R)(IC50valuesare73and100nMrespectively).InhibitsreceptorautophosphorylationanddownstreamMEK1/2andAktsignaling.InducesG1arrestandapoptosisinML-1cells;alsoinhibitscellproliferationinmultipletumortypes.ReversesEMTthroughtheattenuationofSnailmRNAexpressioninMCF10AcelloverexpressingIGF1R.
CompoundLibraries
BMS536924isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 479.96 |
| Formula | C25H26ClN5O3 |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 468740-43-4 |
| PubChemID | 6077765 |
| InChIKey | DXEATJQGQHDURZ-DEDYPNTBSA-N |
| Smiles | O=C1NC=CC(NC[C@H](C5=CC=CC(Cl)=C5)O)=C1C3=NC2=CC(N4CCOCC4)=CC(C)=C2N3 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 48 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight479.96.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.08mL | 10.42mL | 20.84mL |
| 5mM | 0.42mL | 2.08mL | 4.17mL |
| 10mM | 0.21mL | 1.04mL | 2.08mL |
| 50mM | 0.04mL | 0.21mL | 0.42mL |
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ProductDatasheets
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