BiologicalActivity
PotentPDGFRfamilyinhibitor(IC50valuesare1.2,2,7.7and10.5nMforKIT,FLT3,PDGFRβandCSF1Rrespectively;Kd=1.3nMforPDGFRα).Exhibits>30-foldselectivityoverapanelofotherkinasesandexhibitsnoactivityagainstcytochromeP450.Causestumorregressionofleukemiacellxenograftsinmice.Alsoreducesjointswellingandinflammationinamousemodelofcollagen-inducedarthritis.Orallyactive.
CompoundLibraries
AC710isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 562.7 |
| Formula | C31H42N6O4 |
| Storage | Storeat+4°C |
| Purity | ≥99%(HPLC) |
| CASNumber | 1351522-04-7 |
| PubChemID | 54760053 |
| InChIKey | JVCWPUFNLFSKFS-UHFFFAOYSA-N |
| Smiles | CC(C2)(C)N(CC)C(C)(C)CC2OC1=CC=C(C(NC3=CC=C(NC(NC4=NOC(C(C)(C)C)=C4)=O)C=C3)=O)N=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 11.25 | 20 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight562.7.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.78mL | 8.89mL | 17.77mL |
| 5mM | 0.36mL | 1.78mL | 3.55mL |
| 10mM | 0.18mL | 0.89mL | 1.78mL |
| 50mM | 0.04mL | 0.18mL | 0.36mL |
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