BiologicalActivity
PotentandselectiveErbB2inhibitor(IC50=10nM).Exhibits500-1000-foldselectivityforErbB2overErbB1andotherrelatedRTKs.InducesG1cellcyclearrestinanErbB2-overexpressinghumancancercellline.Promotestumorapoptosis.Inducestumorregressioninahumantumorxenograftmodel.Displaysnoapparenttoxiceffectoncardiactissue.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc.
ExternalPortalInformation
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofCP-724714isreviewedonthechemicalprobeswebsite.
TechnicalData
| M.Wt | 469.53 |
| Formula | C27H27N5O3 |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 383432-38-0 |
| PubChemID | 9874913 |
| InChIKey | LLVZBTWPGQVVLW-SNAWJCMRSA-N |
| Smiles | CC1=CC(NC2=NC=NC3=CC=C(/C=C/CNC(COC)=O)C=C32)=CC=C1OC4=CC=C(C)N=C4 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.95 | 100 | |
| ethanol | 46.95 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight469.53.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.13mL | 10.65mL | 21.3mL |
| 5mM | 0.43mL | 2.13mL | 4.26mL |
| 10mM | 0.21mL | 1.06mL | 2.13mL |
| 50mM | 0.04mL | 0.21mL | 0.43mL |
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