Identification | Back Directory | [Name]
Nelotanserin | [CAS]
380449-54-7 | [Synonyms]
Melflufen hydrochloride ethyl (2S)-2-[[(2S)-2-amino-3-[4-[bis(2-chloroethyl)amino]phenyl]propanoyl]amino]-3-(4-fluorophenyl)propanoate | [Molecular Formula]
C24H31Cl3FN3O3 | [MOL File]
380449-54-7.mol | [Molecular Weight]
534.88 |
Hazard Information | Back Directory | [Uses]
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[1][2][3]. | [in vivo]
Melflufen (Melphalan flufenamide) hydrochloride (3 mg/kg; i.v.; twice-weekly for two weeks) shows anti-MM activity in xenograft mouse model[1]. Animal Model: | CB-17 SCID mice (human plasmacytoma MM.1S xenograft mouse model)[1] | Dosage: | 3 mg/kg | Administration: | 1.v.; twice-weekly for two weeks | Result: | Significantly inhibited MM tumor growth and prolonged survival of mice.
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| [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. DOI:10.1158/1078-0432.CCR-12-3752 [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. DOI:10.1111/bjh.14065 [3] McAndrews KM, et, al. Mechanisms associated with biogenesis of exosomes in cancer. Mol Cancer. 2019 Mar 30;18(1):52. DOI:10.1186/s12943-019-0963-9 |
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