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.
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- Purity: 95.46%
- CAS No.: 380449-51-4
- 화학식: C24H30Cl2FN3O3
- 분자량:498.42
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보관:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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- References
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Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Lymphoma cell line | IC50 |
0.011 μM
Compound: Melflufen
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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
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[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.
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Cell Line:Multiple myeloma cells: MM.1S, INA-6, RPMI-8226, MM.1R, Dox-40, ARP-1, ANBL-6 cells
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Concentration:0.5, 1, 3, 5, 10 μM
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Incubation Time:24 hours
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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.
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Animal Model:CB-17 SCID mice (human plasmacytoma MM.1S xenograft mouse model)[1]
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Dosage:3 mg/kg
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Administration:I.v.; twice-weekly for two weeks
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Result:Significantly inhibited MM tumor growth and prolonged survival of mice.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 380449-51-4
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Appearance Oil
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분자량 498.42
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화학식 C24H30Cl2FN3O3
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Color Colorless to light yellow
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Synonyms
Melphalan flufenamide
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
2022 Feb 10;13(2):136. PMID: 35145058
순도&문서
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Data Sheet (271 KB)
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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)
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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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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