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.Wt | 532.57 |
| Formula | C27H29FN8O3 |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1116235-97-2 |
| PubChemID | 25182616 |
| InChIKey | HZTYDQRUAWIZRE-UHFFFAOYSA-N |
| Smiles | O=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
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.26 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight532.57.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.88mL | 9.39mL | 18.78mL |
| 5mM | 0.38mL | 1.88mL | 3.76mL |
| 10mM | 0.19mL | 0.94mL | 1.88mL |
| 50mM | 0.04mL | 0.19mL | 0.38mL |
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ProductDatasheets
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