Name: Aminopterin
Price: 191.00 USD

- Overview
  - Aminopterin is a 4-amino derivative of folic acid and a folic acid antagonist. It is a synthetic derivative of pterin. It has both mmunosuppressive properties and anti-cancer properties and can be used for apoptosis research. The compound was discovered by Dr. Subbarow in 1947 and was first used for pediatric leukemia, marketed by Lederle Laboratories (Pearl River, New York).
    Aminopterin is considered a dangerous good. Quantities above 1 g may be subject to additional shipping fees. Please contact us for questions.
    
    Please contact us at for specific academic pricing.
    
    Background
    
    Aminopterin is transported into cells via the folate transporter. Once inside the cell, it is converted to polyglutamate metabolite that binds to dihydrofolate reductase by competing for the folate binding site and inhibits its activity. It blocks tetrahydrofolate synthesis. This results in depletion of nucleotide precursors, which results in inhibition of DNA, RNA, and protein synthesis. Aminopterin-polyglutamate degrades intracellularly via y-glutamyl hydrolase.
- Properties
  - CAS Number
    
    54-62-6
    
    Molecular Formula
    
    C19H20N8O5
    
    Molecular Weight
    
    440.41
    
    Solubility
    
    Soluble in DMSO and methanol. Slightly soluble in water.
    
    Other Properties
    
    Source: Synthetic
    
    * For research use only
- Applications
  - Application Description
    
    Eukaryotic Cell Culture Applications: The antifolate Aminopterin is used in selection media, such as HAT medium (hypoxanthine-aminopterin-thymidine medium), particularly for the development of hybridomas, which secrete monoclonal antibodies. It acts as a folate metabolism inhibitor. The use of HAT medium is a form of selection for cells containing working TK (thymidine kinase) and HGRPT (hypoxanthine-guanine phosphoribosyltransferase). Aminopterin, via its blockage of the de novo pathway, forces the cells to use the salvage pathway. Hypoxanthine and thymidine are converted by TK and HGRPT but if either of these enzymes is missing as is myeloma cells, then purine or pyrimidine synthesis is blocked and the cells die. Hybrid cells (myeloma-spleen hybrids) can survive as they inherited the enzyme from the lymphocyte parent.
    
    Cancer Applications: A virtual screening model was used to screen multiple target inhibitors for breast cancer, and may act as a potential inhibitor for improving endocrine therapies for breast cancer (Dai et al, 2021).