1. Cell Cycle/DNA Damage
    Apoptosis
  2. DNA Alkylator/Crosslinker
    Apoptosis
  3. Melflufen

Melflufen (Synonyms: Melphalan flufenamide)

Cat. No.: HY-105019
Handling Instructions

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.

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Melflufen Chemical Structure

Melflufen Chemical Structure

CAS No. : 380449-51-4

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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].

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.
Molecular Weight

498.42

Formula

C₂₄H₃₀Cl₂FN₃O₃

CAS No.

380449-51-4

SMILES

O=C(OCC)[[email protected]](CC1=CC=C(F)C=C1)NC([[email protected]](CC2=CC=C(N(CCCl)CCCl)C=C2)N)=O

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

MelflufenMelphalan flufenamideDNA Alkylator/CrosslinkerApoptosismultiplemyelomasurvivalMM.1ScellsDNAdamageangiogenesisgrowthInhibitorinhibitorinhibit

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