BiologicalActivity
Highaffinity,potentandselectiveHsp90inhibitor(Ki=0.2nMandIC50=1.1nM).ExhibitsselectivityforHsp90overGrp94andTRAP1(Kivaluesare61and255nMrespectively)andhasnoeffect(IC50>10μM)againstapanelof285kinases.DegradesHer-2inMCF-7breastcancercells(EC50=14nM).BlockstumorgrowthandinducespartialtumorregressioninanN87gastrictumormousemodel.AlsoinhibitsLPS-inducedTNFαreleaseinanLPSshockmousemodelandsuppressesdiseasedevelopmentinaratmodelofcollagen-inducedarthritis.Exhibits<20-foldefficacyoverBIIB021(Cat.No.4608)inmice.Orallyavailableandbrainpenetrant.
CompoundLibraries
EC144isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 413.9 |
| Formula | C21H24ClN5O2 |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 911397-80-3 |
| PubChemID | 11517212 |
| InChIKey | VOASEWXFCTZRDF-UHFFFAOYSA-N |
| Smiles | ClC1=C2C(N(CC3=C(C)C(OC)=C(C)C=N3)C=C2C#CCC(C)(C)O)=NC(N)=N1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.39 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight413.9.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.42mL | 12.08mL | 24.16mL |
| 5mM | 0.48mL | 2.42mL | 4.83mL |
| 10mM | 0.24mL | 1.21mL | 2.42mL |
| 50mM | 0.05mL | 0.24mL | 0.48mL |
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ProductDatasheets
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