Melflufen (Melphalan flufenamide, J1) is a novel dipeptide and alkylating prodrug of melphalan, inhibits angiogenesis in vitro and in vivo; shows cytotoxic activity against lymphoma cell lines with IC50 of 0.011-0.92 uM, also shows significantly lower IC50 than melphalan in multiple myeloma cells; induces apoptosis even in melphalan- and bortezomib-resistant multiple myeloma cells.
Phase 3 Clinical
An alkylating agent used to treat cancer that has been previously used in the palliation of a wide variety of neoplastic diseases.
An alkylating agent used as a treatment of some brain cancers, astrocytoma and glioblastoma; a prodrug and an imidazotetrazine derivative of the alkylating agent dacarbazine.
A synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic and immunosuppressive activities; used to treat cancers and autoimmune diseases.
A small molecule DNA intercalater with antineoplastic activity, does not exhibit cardiotoxicity compared with doxorubicin; induces both protein-associated DNA single-strand breaks and DNA-protein crosslinks in cancer cells.
A potent and selective hypoxia-activated phosphoramidate DNA cross-linking mustard; selectively potent under hypoxia and stable to liver microsomes; inhibits H246 cells and HT29 cells with IC50 of 0.1 uM and 0.2 uM respectively; active in an in vivo MIA PaCa-2 pancreatic cancer orthotopic xenograft model.
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