120368-87-8

Basic information

• Product Name: tetraethyl N-(4-<(<2,4-diamino-6-pteridinyl>methyl) methyl-amino>benzoyl)-3-amino-3-ethoxycarbonylpropylidene-1,1-bisphosphonate
• Synonyms: tetraethyl N-(4-<(<2,4-diamino-6-pteridinyl>methyl) methyl-amino>benzoyl)-3-amino-3-ethoxycarbonylpropylidene-1,1-bisphosphonate
• CAS NO: 120368-87-8
• Molecular Weight: 710.664
• Mol File: 120368-87-8.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: tetraethyl N-(4-<(<2,4-diamino-6-pteridinyl>methyl) methyl-amino>benzoyl)-3-amino-3-ethoxycarbonylpropylidene-1,1-bisphosphonate(CAS DataBase Reference)
• NIST Chemistry Reference: tetraethyl N-(4-<(<2,4-diamino-6-pteridinyl>methyl) methyl-amino>benzoyl)-3-amino-3-ethoxycarbonylpropylidene-1,1-bisphosphonate(120368-87-8)
• EPA Substance Registry System: tetraethyl N-(4-<(<2,4-diamino-6-pteridinyl>methyl) methyl-amino>benzoyl)-3-amino-3-ethoxycarbonylpropylidene-1,1-bisphosphonate(120368-87-8)

Safety Data

• Hazardous Substances Data: 120368-87-8(Hazardous Substances Data)

Upstream product

• 120355-33-1 4,4-Bis-(diethoxy-phosphoryl)-2-{4-[methyl-(2,2,2-trichloro-ethoxycarbonyl)-amino]-benzoylamino}-butyric acid ethyl ester 
• 120355-30-8 2-amino-4,4-bis(diethylphosphono)butanoic acid ethyl ester 
• 52853-40-4 6-bromomethyl-2,4-diaminopteridine hydrobromide 
• 120355-34-2 tetraethyl 3-ethoxycarbonyl-N-<4-(methylamino)benzoyl>-3-aminopropylidene-1,1-bisphosphonate 

Relevant articles and documents

A study of the delivery-targeting concept applied to antineoplastic drugs active on human osteosarcoma. I. Synthesis and biological activity in nude mice carrying human osteosarcoma xenografts of gem-bisphosphonic methotrexate analogues

With the aim of verifying the concept of osteotic vectorisation, synthesis of three methotrexate (MTX) gem-diphosphonic analogues (compounds A, B and C) was performed. These molecules were tested on BALB/c and NIH III mice previously grafted with subcutaneous implants of OHS, TTX p7 and/or TTX p11 human osteosarcoma cell lines. Antineoplasic activity of compound B and C (active compounds) was compared to the activity for MTX alone and to activity of compound A (inactive compound). Compounds B and C exhibited an increased antineoplasic activity compared to MTX alone and to compound A. At equimolar doses, compound B was found to be 5-6-fold more active than MTX given alone. We have discussed the concept of osteotic vectorisation of compound B, which could be regarded as a prodrug.