BiologicalActivity
Potentinhibitorofepidermalgrowthfactorreceptor(EGFR)tyrosinekinase(IC50=3nM).Displays~100-foldlowerpotencyagainstErbB2(IC50=290nM)andisselectiveoverarangeofotherrelatedtyrosinekinases(IC50>10μM).BlocksdownstreamEGFRsignalingeventssuchasMAPKK/MAPKactivation.OraladmiNISTrationinhibitsgrowthofestablishedhumanxenograftsinathymicmice.
CompoundLibraries
BIBU1361dihydrochlorideisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 516.87 |
| Formula | C22H27ClFN7.2HCl |
| Storage | Desiccateat+4°C |
| Purity | ≥97%(HPLC) |
| CASNumber | 793726-84-8 |
| PubChemID | 46861539 |
| InChIKey | ZNNWCQCQUKAMGL-UHFFFAOYSA-N |
| Smiles | Cl.Cl.CCN(CC)CC1CCN(CC1)C1=NC=C2N=CN=C(NC3=CC(Cl)=C(F)C=C3)C2=N1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 12.92 | 25 | |
| ethanol | 2.58 | 5 | |
| water | 51.69 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight516.87.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.93mL | 9.67mL | 19.35mL |
| 5mM | 0.39mL | 1.93mL | 3.87mL |
| 10mM | 0.19mL | 0.97mL | 1.93mL |
| 50mM | 0.04mL | 0.19mL | 0.39mL |
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ProductDatasheets
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