BiologicalActivity
Potent,selectiveandATP-competitiveinhibitorofMETkinase(IC50valuesare9,68,200,1400,3000,3800and6000nMforMET,Ron,Flk-1,c-abl,FGFR1,EGFRandc-srcrespectivelyand>10000nMforIGF-IR,PDGFR,AURORA2,PKA,PKBα,p38α,MK2andMK3).Antitumoragent;inhibitstumOrigenicityandangiogenesisinmouselungcancerxenografts.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc.
CompoundLibraries
PHA665752isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxI.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 641.61 |
| Formula | C32H34Cl2N4O4S |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 477575-56-7 |
| PubChemID | 10461815 |
| InChIKey | OYONTEXKYJZFHA-SSHUPFPWSA-N |
| Smiles | ClC1=C(CS(C2=CC(/C(C(N4)=O)=C/C3=C(C)C(C(N5CCC[C@@H]5CN6CCCC6)=O)=C(C)N3)=C4C=C2)(=O)=O)C(Cl)=CC=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 64.16 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight641.61.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.56mL | 7.79mL | 15.59mL |
| 5mM | 0.31mL | 1.56mL | 3.12mL |
| 10mM | 0.16mL | 0.78mL | 1.56mL |
| 50mM | 0.03mL | 0.16mL | 0.31mL |
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