Melflufen(Synonyms: Melphalan flufenamide)

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Melflufen (Synonyms: Melphalan flufenamide)

Melflufen (Melphalan flufenamide)，Melphalan 的一种二肽前体药物，是一种烷基化剂。Melflufen 对多发性骨髓瘤细胞具有抗肿瘤活性，并抑制血管生成。Melflufen 对骨髓瘤细胞 DNA 不可逆损伤及细胞毒作用。

Melflufen(Synonyms: Melphalan flufenamide)

Melflufen Chemical Structure

CAS No. : 380449-51-4

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Melflufen 的其他形式现货产品:

Melflufen hydrochloride

生物活性

Melflufen (Melphalan flufenamide), a dipeptide prodrug 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[1][2][3].

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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.

体内研究
(In Vivo)

Melflufen (Melphalan flufenamide) (3 mg/kg; i.v.; twice-weekly for two weeks) shows anti-MM activity in xenograft mouse model[1].

Shanghai Jinpan Biotech Co Ltd 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.

Clinical Trial

分子量

498.42

Formula

C24H30Cl2FN3O3
CAS 号

380449-51-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

    [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.

    [3]. McAndrews KM, et, al. Mechanisms associated with biogenesis of exosomes in cancer. Mol Cancer. 2019 Mar 30;18(1):52.

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