BiologicalActivity
PotentPAK4inhibitor(IC50=1.3nM;Kd=2.7nM).Inhibitsproliferationandanchorage-independentgrowthofapaneloftumorcelllinesinvitro.SuppressesgrowthofhumanHCT116andA549tumorcellxenograftsinmice.Orallyavailable.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc
ExternalPortalInformation
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofPF3758309isreviewedontheChemicalProbeswebsite.
TechnicalData
| M.Wt | 563.55 |
| Formula | C25H30N8OS.2HCl |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| PubChemID | 91885498 |
| InChIKey | BTVSNRMSUYBDRT-JQDLGSOUSA-N |
| Smiles | CN(C[C@H](C1=CC=CC=C1)NC(N2CC3=C(C2(C)C)NN=C3NC4=C5SC=CC5=NC(C)=N4)=O)C.Cl.Cl |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 56.35 | 100 | |
| water | 56.35 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight563.55.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.77mL | 8.87mL | 17.74mL |
| 5mM | 0.35mL | 1.77mL | 3.55mL |
| 10mM | 0.18mL | 0.89mL | 1.77mL |
| 50mM | 0.04mL | 0.18mL | 0.35mL |

