BiologicalActivity
Potent,irreversibleinhibitorofErbB2(HER2)andEGFR(IC50valuesare33and34nMrespectively).Suppressesligand-inducedEGFRautophosphorylationandcellproliferationinNCI-H1975cellscontainingL858RandT790Mmutations.CircumventsmechanismsofresistancetoIressa(Cat.No.3000)innon-small-celllungcancercells.
CompoundLibraries
HKI357isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxI.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
M.Wt | 574.05 |
Formula | C31H29ClFN5O3 |
Storage | Storeat-20°C |
Purity | ≥98%(HPLC) |
CASNumber | 848133-17-5 |
PubChemID | 11238512 |
InChIKey | NERXPXBELDBEPZ-RMKNXTFCSA-N |
Smiles | O=C(/C=C/CN(C)C)NC1=C(OCC)C=C(N=CC(C#N)=C2NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)C2=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
Solvent | MaxConc.mg/mL | MaxConc.mM | |
---|---|---|---|
Solubility | |||
DMSO | 57.4 | 100 | |
ethanol | 14.35 | 25 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight574.05.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
---|---|---|---|
1mM | 1.74mL | 8.71mL | 17.42mL |
5mM | 0.35mL | 1.74mL | 3.48mL |
10mM | 0.17mL | 0.87mL | 1.74mL |
50mM | 0.03mL | 0.17mL | 0.35mL |