MolecularWeight: | 717.98 |
Formula: | C39H67N5O7 |
Purity: | ≥95% |
CAS#: | 474645-27-7 |
Solubility: | DMSOupto20mM |
ChemicalName: | (S)-N-((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1S,2R)-1-hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxoheptan-4-yl)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamide |
Storage: | Powder:-20oC1year |
MonomethylauristatinE(MMAE,vedotin)isaverypotentanti-mitoticagentthatinhibitscelldivisionbyblockingthepolymerisationoftubulin.Becauseoftssupertoxicity,itcannotbeusedasadrugitself.Inrecentcancertherapydevelopments,itislinkedtoamonoclonalantibody(mAb)thatrecognizesapecificMarkerexpressionincancercellsanddirectsMMAEtothecancercells.ThelinkerlinkingMMAEtothemonoclonalantibodyisstableinextracellularfluid,butiscleavedbycathepsinoncetheantibody-drug-conjugate/ADChasboundtothespecificcancercellantigenandenteredthecancercell,thusreleasingtheoxicMMAEandactivatingthepotentanti-mitoticmechanism.
Reference:
- 1.FranciscoJA,etal.cAC10-vcMMAE,ananti-CD30-monomethylauristatinEconjugatewithpotentandselectiveantitumoractivity.(2003)Blood.102(4):1458-65.
- 2.JunutulaJR,etal.Site-specificconjugationofacytotoxicdrugtoanantibodyimprovesthetherapeuticindex.(2008)NatBiotechnol.26(8):925-32.
- 3.AsundiJ,etal.Anantibody-drugconjugatetargetingtheendothelinBreceptorforthetreatmentofmelanoma.(2011)ClinCancerRes.17(5):965-75.
- 4.YounesA,etal.ResultsofaPivotalPhaseIIStudyofBrentuximabVedotinforPatientsWithRelapsedorRefractoryHodgkin"sLymphoma.(2012)JClinOncol.30(18):2183-9.
- 5.http://en.wikipedia.org/wiki/Monomethyl_auristatin_E
MMAE_spec.pdf
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