Melflufen
Based on 1 publication(s) in Google Scholar
Melflufen (Melphalan flufenamide), a dipeptide proagent 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.
For research use only. We do not sell to patients.
- Purity : 95.46%
- CAS No.: 380449-51-4
- Formula: C24H30Cl2FN3O3
- Molecular Weight:498.42
-
Storage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Melflufen
More
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Lymphoma cell line | IC50 |
0.011 μM
Compound: Melflufen
|
Cytotoxicity against patient-derived human lymphoma cells assessed as cell growth inhibition incubated for 72 hrs by FMCA assay
Cytotoxicity against patient-derived human lymphoma cells assessed as cell growth inhibition incubated for 72 hrs by FMCA assay
|
[PMID: 35665692] |
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].
Melphalan 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.
-
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
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:I.v.; twice-weekly for two weeks
-
Result:Significantly inhibited MM tumor growth and prolonged survival of mice.
- Human pluripotent stem cell endothelial-cell differentiation
- Vascular/Branching Fractal Analysis
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Endothelial Tube Formation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Endothelial Cell Migration/Angiogenic Sprouting Assay
- Genotoxicity/Mutagenicity Study
- Cell Viability Determination by MTT Colorimetric Assay
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 380449-51-4
-
Appearance Oil
-
Molecular Weight 498.42
-
Formula C24H30Cl2FN3O3
-
Color Colorless to light yellow
-
Synonyms
Melphalan flufenamide
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Cell Death Dis
2022 Feb 10;13(2):136. PMID: 35145058
Solvent & Solubility
In Vitro:
DMSO : ≥ 50 mg/mL (100.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.02 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.02 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
-
Data Sheet (274 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
[1]. Chauhan D, et al. In vitro and in vivo antitumor activity of a novel alkylating agent, melphalan-flufenamide, against multiple myeloma cells. Clin Cancer Res. 2013;19(11):3019-3031. [Content Brief]
[2]. Ray A, et al. A novel alkylating agent Melflufen induces irreversible DNA damage and cytotoxicity in multiple myeloma cells. Br J Haematol. 2016;174(3):397-409. [Content Brief]
[3]. McAndrews KM, et, al. Mechanisms associated with biogenesis of exosomes in cancer. Mol Cancer. 2019 Mar 30;18(1):52. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0063 mL | 10.0317 mL | 20.0634 mL | 50.1585 mL |
| 5 mM | 0.4013 mL | 2.0063 mL | 4.0127 mL | 10.0317 mL | |
| 10 mM | 0.2006 mL | 1.0032 mL | 2.0063 mL | 5.0158 mL | |
| 15 mM | 0.1338 mL | 0.6688 mL | 1.3376 mL | 3.3439 mL | |
| 20 mM | 0.1003 mL | 0.5016 mL | 1.0032 mL | 2.5079 mL | |
| 25 mM | 0.0803 mL | 0.4013 mL | 0.8025 mL | 2.0063 mL | |
| 30 mM | 0.0669 mL | 0.3344 mL | 0.6688 mL | 1.6719 mL | |
| 40 mM | 0.0502 mL | 0.2508 mL | 0.5016 mL | 1.2540 mL | |
| 50 mM | 0.0401 mL | 0.2006 mL | 0.4013 mL | 1.0032 mL | |
| 60 mM | 0.0334 mL | 0.1672 mL | 0.3344 mL | 0.8360 mL | |
| 80 mM | 0.0251 mL | 0.1254 mL | 0.2508 mL | 0.6270 mL | |
| 100 mM | 0.0201 mL | 0.1003 mL | 0.2006 mL | 0.5016 mL |
Melflufen Related Classifications
HY-105019 Related Classifications
Powered by Bioz