CAS380449-51-4 Melflufen

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CAS380449-51-4 Melflufen
Details
CAS: 380449-51-4
Chemical name: Ethyl (2S)-2-[[(2S)-3-[4-[bis(2-chloroethyl)amino]phenyl]-2-aminopropanoyl]amino]-3-(4-fluorophenyl)propanoate
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Related documents
COA/MS/HPLC Report
Compound Dissolution and Storage Guide
Category
Peptide-Drug Conjugate (PDC)
Category
Pharmaceutical Peptides
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Description

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Product name CAS380449‑51‑4 Melflufen
Chemical name Ethyl (2S)-2-[[(2S)-3-[4-[bis(2-chloroethyl)amino]phenyl]-2-aminopropanoyl]amino]-3-(4-fluorophenyl)propanoate
Three letter sequence H-Melphalan-Phe(4-F)-OEt
Purity (HPLC, %) 95%/98%/99%
Molecular formula C₂₈H₃₀Cl₂FN₃O₄
Molecular weight (Da) 566.46

 

Product Basic Information Table

 

Product Standard English Name Product Abbreviation / Alias Function Tags (comma-separated) Amino Acid Full Name Sequence Molecular Formula Exact Molecular Weight (Da) Average Molecular Weight (Da) N-terminal Modification C-terminal Modification Sequence Length (aa)
Melflufen Melphalan flufenamide; Pepaxto; CAS 380449-51-4; Peptide-conjugated alkylating agent Peptide-drug conjugate,DNA alkylating agent,Multiple myeloma therapy,Antitumor cytotoxicity,Drug-resistant tumor research 4-Bis(2-chloroethyl)amino-L-phenylalanine-L-4-fluorophenylalanine (C-terminal ethyl ester) C₂₈H₃₀Cl₂FN₃O₄ 565.16 566.46 Bis(2-chloroethyl)amino modification on phenyl ring Ethyl ester modification 2

 

Physicochemical Solubility & Storage Parameters

 

Product Code Appearance Long-term Storage Conditions Short-term Storage Conditions Liquid Stability Solid Powder Stability
PDC-MEL001 white powder Store at -20℃, strictly protected from light, sealed and dry, aliquoted; avoid repeated freeze-thaw cycles and moisture Solid powder stable for 2 years sealed and dry at 2-8℃; DMSO stock solution stable for 1 month at -20℃ in dark DMSO solution stable for 72 h at 4℃; nitrogen mustard group and ester bond are prone to hydrolysis in aqueous solution, prepare freshly before use Stable for 3 years at -20℃ under dry & dark conditions

 

Functional Description

 

Product Code Frontend Short Summary (for search list display) Detailed Biological Function Description Applicable Research Areas (comma-separated) Target / Receptor
PDC-MEL001 Aminopeptidase-activated peptide-conjugated alkylating agent with high tumor-selective cytotoxicity, applied in relapsed/refractory multiple myeloma and drug-resistant tumor research Melflufen (brand name Pepaxto) is the first approved peptide-drug conjugate (PDC) alkylating agent, consisting of a melphalan active moiety linked to L-4-fluorophenylalanine ethyl ester via a peptide bond. It is rapidly hydrolyzed by aminopeptidases highly expressed on tumor cells, selectively releasing high concentrations of active melphalan inside tumor cells. The bis(2-chloroethyl)amino group alkylates DNA bases, inducing DNA interstrand crosslinks and double-strand breaks, causing cell cycle arrest and tumor cell apoptosis. Compared with conventional melphalan, it achieves higher tumor enrichment and lower systemic toxicity, and retains cytotoxicity against multiple myeloma cells resistant to proteasome inhibitors and immunomodulatory drugs. Clinically approved for relapsed/refractory multiple myeloma, it serves as a core tool molecule for hematological oncology pharmacology, drug resistance mechanism research and peptide-drug conjugate development. Hematological oncology research,Multiple myeloma research,Drug-resistant tumor research,Peptide-drug conjugate development,DNA damage repair researchresearch DNA alkylation damage; Apoptosis pathway; Aminopeptidase-activated prodrug

 

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