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Melflufen is a prodrug form of the DNA alkylating agent melphalan (Item No. 16665).1,2 Melflufen induces apoptosis and inhibits growth in MM.1R, RPMI-8226, and melphalan-resistant RPMI-8226/LR5 multiple myeloma cells in a concentration-dependent manner.1 It induces DNA damage and inhibits VEGF-induced migration of MM.1S multiple myeloma cells and angiogenesis in human umbilical vascular endothelial cells (HUVECs). Melflufen reduces proliferation and induces cell cycle arrest at the G2/M phase in KM-H2 and SU-DHL-10 lymphoma cells (IC50s = 0.22 and 0.77 µM, respectively).2 In vivo, Melflufen reduces tumor growth and increases survival in DoHH2 lymphoma and MM.1S mouse xenograft models.1,2 Formulations containing melflufen have been used in the treatment of refractory multiple myeloma.
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1. In vitro and in vivo antitumor activity of a novel alkylating agent, melphalan-
2. In vitro and in vivo activity of melflufen (J1) in lymphoma. BMC Cancer 16, 263 (2016).