380449-51-4
380449-51-4 structure
- Name: Melflufen
- Chemical Name: ethyl (2S)-2-[[(2S)-2-amino-3-[4-[bis(2-chloroethyl)amino]phenyl]propanoyl]amino]-3-(4-fluorophenyl)propanoate
- CAS Number: 380449-51-4
- Molecular Formula: C24H30Cl2FN3O3
- Molecular Weight: 498.41800
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2017-02-05 08:33:48
- Modify Date: 2025-08-25 12:35:20
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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].
| Name | ethyl (2S)-2-[[(2S)-2-amino-3-[4-[bis(2-chloroethyl)amino]phenyl]propanoyl]amino]-3-(4-fluorophenyl)propanoate |
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| 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 |
| 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]. |
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| 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 |
| Molecular Formula | C24H30Cl2FN3O3 |
|---|---|
| Molecular Weight | 498.41800 |
| Exact Mass | 497.16500 |
| PSA | 88.15000 |
| LogP | 4.81070 |