| Description | Melflufen (Melphalan flufenamide) hydrochloride, an alkylating agent and dipeptide prodrug of Melphalan, exhibits antitumor activity by inducing irreversible DNA damage and cytotoxicity in multiple myeloma (MM) cells, while also inhibiting angiogenesis. |
| In vitro | Melflufen (Melphalan flufenamide) hydrochloride (0.5-10 μM; 24 hours) decreases viability of MM.1S, INA-6, RPMI-8226, MM.1R, Dox-40, ARP-1, and ANBL-6 cells in a concentration-dependent manner[1]. Melflufen hydrochloride induces apoptosis in MM.1S cells[1]. Melflufen hydrochloride also is a potent activator of exosome secretion[3]. Cell Viability Assay[1]Cell Line: Multiple myeloma cells: MM.1S, INA-6, RPMI-8226, MM.1R, Dox-40, ARP-1, ANBL-6 cells Concentration: 0.5, 1, 3, 5, 10 μM Incubation Time: 24 hours Result: A significant concentration-dependent decrease in viability of all cell lines was observed. |
| In vivo | Melflufen (Melphalan flufenamide) hydrochloride (3 mg/kg; i.v.; twice-weekly for two weeks) shows anti-MM activity in xenograft mouse model[1]. Animal Model: CB-17 SCID mice (human plasmacytoma MM.1S xenograft mouse model)[1]Dosage: 3 mg/kg Administration: 1.v.; twice-weekly for two weeks Result: Significantly inhibited MM tumor growth and prolonged survival of mice. |
| Synonyms | Melflufen hydrochloride, Melphalan flufenamide hydrochloride |
| molecular weight | 534.88 |
| Molecular formula | C24H31Cl3FN3O3 |
| CAS | 380449-54-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Chauhan D, et al. In vitro and in vivo antitumor activity of a novel alkylating agent, melphalan-flufenamide, against multiple myeloma cells. Clin Cancer Res. 2013;19(11):3019-3031. 2. Ray A, et al. A novel alkylating agent Melflufen induces irreversible DNA damage and cytotoxicity in multiple myeloma cells. Br J Haematol. 2016;174(3):397-409. 3. McAndrews KM, et, al. Mechanisms associated with biogenesis of exosomes in cancer. Mol Cancer. 2019 Mar 30;18(1):52. |