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Melflufen (Melphalan flufenamide), a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen exhibits significant antitumor activity against multiple myeloma (MM) cells and has been shown to inhibit angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells, thereby contributing to its antitumor efficacy. At equivalent molar concentrations, both the salt and free forms of Melflufen exhibit comparable biological activity. However, the salt form, Melflufen hydrochloride, typically demonstrates enhanced water solubility and stability, which may contribute to its increased therapeutic potential.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $239 | - | In Stock | |
| 5 mg | $596 | - | In Stock | |
| 10 mg | $793 | - | In Stock | |
| 25 mg | $1,260 | - | In Stock | |
| 50 mg | $1,630 | - | In Stock | |
| 100 mg | $1,980 | - | In Stock |
| Description | Melflufen (Melphalan flufenamide), a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen exhibits significant antitumor activity against multiple myeloma (MM) cells and has been shown to inhibit angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells, thereby contributing to its antitumor efficacy. At equivalent molar concentrations, both the salt and free forms of Melflufen exhibit comparable biological activity. However, the salt form, Melflufen hydrochloride, typically demonstrates enhanced water solubility and stability, which may contribute to its increased therapeutic potential. |
| Targets&IC50 | Lymphoma cell:0.011 μM |
| In vitro | Methods: Multiple myeloma cell lines including MM.1S, INA-6, RPMI-8226, MM.1R, Dox-40, ARP-1, and ANBL-6 were treated with Melflufen (0.5-10 μM, 24 hours), and cell viability was assessed via MTT assay. Results: Melflufen demonstrated significant cytotoxicity across all the aforementioned multiple myeloma cell lines.[4] |
| In vivo | Methods: Melflufen (3 mg/kg, twice weekly for 2 weeks) was administered intravenously to CB-17 SCID mice, and tumor growth and survival were observed. Results: Melflufen significantly inhibited MM tumor growth in vivo and prolonged the survival time of the mice.[4] |
| Synonyms | Prodrug J-1 |
| Molecular Weight | 498.42 |
| Formula | C24H30Cl2FN3O3 |
| Cas No. | 380449-51-4 |
| Smiles | N(CCCl)(CCCl)C1=CC=C(C[C@@H](C(N[C@@H](CC2=CC=C(F)C=C2)C(OCC)=O)=O)N)C=C1 |
| Relative Density. | 1.265 g/cm3 (Predicted) |
| Sequence | H-Phe(Unk)-Phe(4-F)-OEt |
| Sequence Short | XX |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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