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

Melflufen hydrochloride (Synonyms: Melphalan flufenamide hydrochloride)

Cat. No.: HY-105019A
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Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells.

For research use only. We do not sell to patients.

Melflufen hydrochloride Chemical Structure

Melflufen hydrochloride Chemical Structure

CAS No. : 380449-54-7

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Description

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

In Vitro

Melflufen (Melphalan flufenamide) hydrochloride (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 hydrochloride induces apoptosis in MM.1S cells[1].

Cell Viability Assay[1]

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) hydrochloride (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: 1.v.; twice-weekly for two weeks
Result: Significantly inhibited MM tumor growth and prolonged survival of mice.
Molecular Weight

534.88

Formula

C₂₄H₃₁Cl₃FN₃O₃

CAS No.

380449-54-7

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.[H]Cl

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Room temperature in continental US; may vary elsewhere.

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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Melflufen hydrochloride
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