BiologicalActivity
Selective,ATP-competitivep38inhibitor(IC50=9nMforp38αinvitro).Displaysapproximately10-foldselectivityforp38αoverp38βand2000-foldselectivityforp38αover20otherkinases.Reducesp38αphosphorylationinmultiplemyelomacellsinvitroandinvivo;activityresultsindecreasedtumorburdenandangiogenesisinmurinemodelsofmultiplemyeloma.Alsoenhancesbortezomib-inducedcytotoxicityagainstmultiplemyelomacells.
CompoundLibraries
SCIO469hydrochlorideisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 549.46 |
| Formula | C27H30ClFN4O3.HCl |
| Storage | Desiccateat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 309913-83-5 |
| PubChemID | 16035045 |
| InChIKey | FOJUFGQLUOOBQP-MCJVGQIASA-N |
| Smiles | O=C(C(N(C)C)=O)C2=CN(C)C1=CC(Cl)=C(C(N3[C@H](C)CN(CC4=CC=C(F)C=C4)[C@@H](C)C3)=O)C=C12.Cl |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 54.95 | 100 | |
| water | 5.49 | 10 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight549.46.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.82mL | 9.1mL | 18.2mL |
| 5mM | 0.36mL | 1.82mL | 3.64mL |
| 10mM | 0.18mL | 0.91mL | 1.82mL |
| 50mM | 0.04mL | 0.18mL | 0.36mL |
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