BiologicalActivity
Selectivecheckpointkinase1(Chk1)inhibitor(Kivaluesare0.49and47nMforChk1andChk2respectively).AbrogatescellcyclearrestatSandG2-Mcheckpoints;sensitizescellstoDNAdamage.Enhancesdocetaxel(Cat.No.4056)efficacyintumorcellsandxenografts.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc.
ExternalPortalInformation
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofPF477736isreviewedonthechemicalprobeswebsite.
CompoundLibraries
PF477736isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 419.48 |
| Formula | C22H25N7O2 |
| Storage | Storeat+4°C |
| Purity | ≥99%(HPLC) |
| CASNumber | 952021-60-2 |
| PubChemID | 16750408 |
| InChIKey | YFNWWNRZJGMDBR-LJQANCHMSA-N |
| Smiles | O=C([C@H](N)C4CCCCC4)NC1=CC3=C(C(C=NNC3=O)=C(C5=CN(C)N=C5)N2)C2=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 31.46 | 75 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight419.48.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.38mL | 11.92mL | 23.84mL |
| 5mM | 0.48mL | 2.38mL | 4.77mL |
| 10mM | 0.24mL | 1.19mL | 2.38mL |
| 50mM | 0.05mL | 0.24mL | 0.48mL |

