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Melflufen

Names

[ CAS No. ]:
380449-51-4

[ Name ]:
Melflufen

[Synonym ]:
UNII-F70C5K4786
Melphalan flufenamide
Melphalan flufenamide [INN]
L-Phenylalanine,4-(bis(2-chloroethyl)amino)-l-phenylalanyl-4-fluoro-,ethyl ester
Prodrug J 1
J 1 (prodrug)
Ethyl (2S)-2-((2S)-2-amino-3-(4-(bis(2-chloroethyl)amino)phenyl)propanamido)-3-(4-fluorophenyl)propanoate
Melflufen

Biological Activity

[Description]:

Melflufen (Melphalan flufenamide), a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells[1][2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> DNA Alkylator/Crosslinker

[In Vitro]

Melflufen (Melphalan flufenamide) (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 induces apoptosis in MM.1S cells[1]. Cell Viability Assay 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) (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: I.v.; twice-weekly for two weeks Result: Significantly inhibited MM tumor growth and prolonged survival of mice.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H30Cl2FN3O3

[ Molecular Weight ]:
498.41800

[ Exact Mass ]:
497.16500

[ PSA ]:
88.15000

[ LogP ]:
4.81070

Related Compounds