BiochemProbe — Life Science Research Reagents

Melflufen free base · Synonyms: Melphalan flufenamide

Melflufen (Melphalan flufenamide), a dipeptide proagent of Melphalan, is an alkylating agent.

For research use only. Not for human or veterinary use.

Research area Cancer
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Description

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 .

Biological activity

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. Melflufen induces apoptosis in MM.1S cells. Melphalan also is a potent activator of exosome secretion. In Vivo Melflufen (Melphalan flufenamide) (3 mg/kg; i.v.; twice-weekly for two weeks) shows anti-MM activity in xenograft mouse model.

Identifiers

SMILES
O=C([C@@H](NC([C@@H](N)CC1=CC=C(C=C1)N(CCCl)CCCl)=O)CC2=CC=C(C=C2)F)OCC
InChIKey
YQZNKYXGZSVEHI-VXKWHMMOSA-N

Specifications

MW (average)
498.4180
Formula
C24H30Cl2FN3O3
CAS No.
380449-51-4
Physical state
Oil
Color
Colorless to light yellow
Shipping
Storage

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.
[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.

Same research area

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