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

Melflufen hydrochloride  (Synonyms: Melphalan flufenamide hydrochloride)

Cat. No.: HY-105019A Purity: 98.73%
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Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide proagent 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

Size Price Stock Quantity
1 mg USD 168 In-stock
5 mg USD 420 In-stock
10 mg USD 700 In-stock
50 mg USD 1900 In-stock
100 mg USD 2900 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Melflufen hydrochloride:

Melflufen hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Melflufen hydrochloride

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide proagent 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][3].

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].
Melflufen hydrochloride also is a potent activator of exosome secretion[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Melflufen hydrochloride Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

534.88

Formula

C24H31Cl3FN3O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(OCC)[C@H](CC1=CC=C(F)C=C1)NC([C@H](CC2=CC=C(N(CCCl)CCCl)C=C2)N)=O.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (62.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 1 mg/mL (1.87 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8696 mL 9.3479 mL 18.6958 mL
5 mM 0.3739 mL 1.8696 mL 3.7392 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 1 mg/mL (1.87 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*The compound is unstable in solutions, freshly prepared is recommended.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.73%

COA (248 KB) LCMS (99 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.8696 mL 9.3479 mL 18.6958 mL 46.7395 mL
DMSO 5 mM 0.3739 mL 1.8696 mL 3.7392 mL 9.3479 mL
10 mM 0.1870 mL 0.9348 mL 1.8696 mL 4.6739 mL
15 mM 0.1246 mL 0.6232 mL 1.2464 mL 3.1160 mL
20 mM 0.0935 mL 0.4674 mL 0.9348 mL 2.3370 mL
25 mM 0.0748 mL 0.3739 mL 0.7478 mL 1.8696 mL
30 mM 0.0623 mL 0.3116 mL 0.6232 mL 1.5580 mL
40 mM 0.0467 mL 0.2337 mL 0.4674 mL 1.1685 mL
50 mM 0.0374 mL 0.1870 mL 0.3739 mL 0.9348 mL
60 mM 0.0312 mL 0.1558 mL 0.3116 mL 0.7790 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Melflufen hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Melflufen380449-54-7Melphalan flufenamideDNA Alkylator/CrosslinkerApoptosismultiplemyelomasurvivalMM.1ScellsDNAdamageangiogenesisgrowthInhibitorinhibitorinhibit

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