Melflufen

Modify Date: 2024-01-06 18:08:10

Melflufen Structure
Melflufen structure
Common Name Melflufen
CAS Number 380449-51-4 Molecular Weight 498.41800
Density N/A Boiling Point N/A
Molecular Formula C24H30Cl2FN3O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Melflufen


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].

 Names

Name ethyl (2S)-2-[[(2S)-2-amino-3-[4-[bis(2-chloroethyl)amino]phenyl]propanoyl]amino]-3-(4-fluorophenyl)propanoate
Synonym More Synonyms

 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
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

 Synonyms

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
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: Melflufen
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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