BiologicalActivity
PotentdualEGFR/ErbB2tyrosinekinaseinhibitor(IC50valuesare0.01and0.014μMrespectively).SelectivelyinhibitsgrowthofhumantumorcellsoverexpressingEGFRandErbB2(IC50valuesare0.11μMforinhibitionofHN5,N87andBT474tumorcelllinesvs.>30μMforinhibitionofnon-tumorcelllineHFF).Inhibitstumorgrowthinvivoby~80%inamurinexenograftmodelfollowingoraladmiNISTration.
LicensingInformation
SoldforresearchpurposesunderagreementfromGlaxoSmithKline.
CompoundLibraries
GW583340dihydrochlorideisalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxI.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 671.03 |
| Formula | C28H25ClFN5O3S2.2HCl |
| Storage | Desiccateat+4°C |
| Purity | ≥97%(HPLC) |
| CASNumber | 1173023-85-2 |
| PubChemID | 16219404 |
| InChIKey | WIMITXDBYLKRKB-UHFFFAOYSA-N |
| Smiles | Cl.Cl.CS(=O)(=O)CCNCC1=NC(=CS1)C1=CC=C2N=CN=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)C2=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 67.1 | 100mMwithgentlewarming |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight671.03.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.49mL | 7.45mL | 14.9mL |
| 5mM | 0.3mL | 1.49mL | 2.98mL |
| 10mM | 0.15mL | 0.75mL | 1.49mL |
| 50mM | 0.03mL | 0.15mL | 0.3mL |
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