| Name | Melflufen |
| Description | Melflufen (Melphalan flufenamide), a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen exhibits significant antitumor activity against multiple myeloma (MM) cells and has been shown to inhibit angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells, thereby contributing to its antitumor efficacy. At equivalent molar concentrations, both the salt and free forms of Melflufen exhibit comparable biological activity. However, the salt form, Melflufen hydrochloride, typically demonstrates enhanced water solubility and stability, which may contribute to its increased therapeutic potential. |
| In vitro | Methods: Multiple myeloma cell lines including MM.1S, INA-6, RPMI-8226, MM.1R, Dox-40, ARP-1, and ANBL-6 were treated with Melflufen (0.5-10 μM, 24 hours), and cell viability was assessed via MTT assay.
Results: Melflufen demonstrated significant cytotoxicity across all the aforementioned multiple myeloma cell lines.[4] |
| In vivo | Methods: Melflufen (3 mg/kg, twice weekly for 2 weeks) was administered intravenously to CB-17 SCID mice, and tumor growth and survival were observed.
Results: Melflufen significantly inhibited MM tumor growth in vivo and prolonged the survival time of the mice.[4] |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Keywords | Prodrug J-1, Melflufen, Melphalan flufenamide | J-1 | J1 | J 1 |
United States
