BiologicalActivity
PotentandselectiveinhibitorofTGF-βtypeIreceptor(ALK5).InhibitsSmad-2phosphorylation(IC50=5.3nM).Exhibitsselectivityoverapanelof27serine/threonineandtyrosinekinasesincludingP38α.AttenuatesTGFβ/Smadsignaling,cellmigration,invasion,lungmetastasisandincreasessurvivalofmicein4TIinvivomodels.Suppressesrenalfibrosisinobstructivenephropathyinvivomodels.
TechnicalData
| M.Wt | 420.47 |
| Formula | C25H20N6O |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 868612-83-3 |
| PubChemID | 11676119 |
| InChIKey | RYKSGWSKILPDDY-UHFFFAOYSA-N |
| Smiles | CC1=NC(C2=C(C3=CC4=C(N=CC=N4)C=C3)NC(CC5=CC(C(N)=O)=CC=C5)=N2)=CC=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| 1eq.HCl | 42.05 | 100 | |
| DMSO | 42.05 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight420.47.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.38mL | 11.89mL | 23.78mL |
| 5mM | 0.48mL | 2.38mL | 4.76mL |
| 10mM | 0.24mL | 1.19mL | 2.38mL |
| 50mM | 0.05mL | 0.24mL | 0.48mL |
MolarityCalculator
ReconstitutionCalculator
Thereconstitutioncalculatorallowsyoutoquicklycalculatethevolumeofareagenttoreconstituteyourvial.Simplyenterthemassofreagentandthetargetconcentrationandthecalculatorwilldeterminetherest.