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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 95.46%
- CAS 番号: 380449-51-4
- 分子式: C24H30Cl2FN3O3
- 分子量:498.42
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保管条件:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 Melflufen
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生物活性
製品説明
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] |
体外実験
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.
体内実験
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.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 380449-51-4
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性状 Oil
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分子量 498.42
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分子式 C24H30Cl2FN3O3
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Color Colorless to light yellow
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別名
Melphalan flufenamide
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)