Melflufen

Research use only, not for human use.

Melflufen ?is a novel dipeptide and alkylating prodrug of melphalan, inhibits angiogenesis in vitro and in vivo; shows cytotoxic activity against lymphoma cell lines with IC50 of 0.011-0.92 uM, also shows significantly lower IC50 than melphalan in multiple myeloma cells.

Melflufen (Melphalan flufenamide, J1)?is a novel dipeptide and alkylating prodrug of melphalan, inhibits angiogenesis in vitro and in vivo; shows cytotoxic activity against lymphoma cell lines with IC50 of 0.011-0.92 uM, also shows significantly lower IC50 than melphalan in multiple myeloma cells; induces apoptosis even in melphalan- and bortezomib-resistant multiple myeloma cells.Blood Cancer Phase 3 Clinical.

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. 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.

Melflufen (Melphalan flufenamide) (3 mg/kg; i.v.; twice-weekly for two weeks) shows anti-MM activity in xenograft mouse model. Animal Model:CB-17 SCID mice (human plasmacytoma MM.1S xenograft mouse model)Dosage:3 mg/kg Administration:I.v.; twice-weekly for two weeks Result:Significantly inhibited MM tumor growth and prolonged survival of mice.

Melphalan flufenamide | J1

Cell Cycle/DNA Damage

DNA Alkylator

DNA Alkylator

Cancer

Blood cancer

380449-51-4

498.42

C24H30Cl2FN3O3

>98% (HPLC)

——

CCOC(=O)C(CC1=CC=C(C=C1)F)NC(=O)C(CC2=CC=C(C=C2)N(CCCl)CCCl)N

ethyl (S)-2-((S)-2-amino-3-(4-(bis(2-chloroethyl)amino)phenyl)propanamido)-3-(4-fluorophenyl)propanoate

(-20℃)

With Ice Pack

≥ 2 years