BiologicalActivity
Potentandselectiveinhibitorofthetransforminggrowthfactor-β(TGF-β)typeIreceptoractivinreceptor-likekinaseALK5(IC50=94nM),anditsrelativesALK4andALK7.SuppressesTGF-β-inducedproliferationofhumanosteosarcomacells.Stimulatesproliferation,differentiationandsheetformationofESC-derivedendothelialcells.InhibitsTGF-β-inducedEMT,migration,invasionandVEGFsecretioninseveralhumancancercelllines.
LicensingInformation
SoldforresearchpurposesunderagreementfromGlaxoSmithKline
CompoundLibraries
SB431542isalsoofferedaspartoftheTocriscreenPlus,TocriscreenKinaseInhibitorToolboxIandTocriscreenStemCellToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 384.39 |
| Formula | C22H16N4O3 |
| Storage | StoreatRT |
| Purity | ≥99%(HPLC) |
| CASNumber | 301836-41-9 |
| PubChemID | 4521392 |
| InChIKey | FHYUGAJXYORMHI-UHFFFAOYSA-N |
| Smiles | NC(=O)C1=CC=C(C=C1)C1=NC(=C(N1)C1=CC=CC=N1)C1=CC2=C(OCO2)C=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.44 | 100 | |
| ethanol | 3.84 | 10 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight384.39.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.6mL | 13.01mL | 26.02mL |
| 5mM | 0.52mL | 2.6mL | 5.2mL |
| 10mM | 0.26mL | 1.3mL | 2.6mL |
| 50mM | 0.05mL | 0.26mL | 0.52mL |
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