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Melflufen

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Catalog No. T33281Cas No. 380449-51-4
Alias Prodrug J-1

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.

Melflufen

Melflufen

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Purity: 97.05%
Catalog No. T33281Alias Prodrug J-1Cas No. 380449-51-4
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
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
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:97.05%
Appearance:Viscous
Color:White
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Product Introduction

Bioactivity
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]
SynonymsProdrug J-1
Chemical Properties
Molecular Weight498.42
FormulaC24H30Cl2FN3O3
Cas No.380449-51-4
SmilesN(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)
SequenceH-Phe(Unk)-Phe(4-F)-OEt
Sequence ShortXX
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
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Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

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This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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