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Melflufen hydrochloride salt form · hydrochloride · Parent Melflufen

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

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

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Description

Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells .

Biological activity

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

Identifiers

SMILES
O=C(OCC)[C@H](CC1=CC=C(F)C=C1)NC([C@H](CC2=CC=C(N(CCCl)CCCl)C=C2)N)=O.[H]Cl
InChIKey
ZCMWSKHHXLCVHI-VROPFNGYSA-N

Specifications

MW (average)
534.8790
Formula
C24H31Cl3FN3O3
CAS No.
380449-54-7
Physical state
Solid
Color
Off-white to light yellow
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder 4°C, sealed storage, away from moisture; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO/H2O

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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