Name: BMS-707035
Price: 212.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 value of 15 nM [1].Retroviral IN is an enzyme produced by a retrovirus (such as HIV) that enables its genetic material to be integrated into the DNA of the infected cell. IN is a key component in the retroviral pre-integration complex (PIC) [1].BMS-707035 is an investigational IN inhibitor. However, the IN mutations V75I, Q148R, V151I, and G163R are found to have resistance to BMS-707035. The inhibition of strand transfer activity by BMS-707035 is overcome when increasing amount of target DNA, so the binding of BMS-707035 to IN and target DNA to IN are mutually exclusive. The four terminal bases at the 5' end of LTR can affect the binding of BMS-707035 to IN [3]. The 3' terminus of the viral LTR can regulate the kinetics of binding and dissociation, which will then retard the rate of BMS-707035 association with IN [2].
    
    [1]. Cotelle P. 3-Hydroxy-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-ones as new HIV-1 integrase inhibitors WO2011046873 A1. Expert Opin. Ther Patents, 2011, 21(11): 1799-1804.
    [2]. Langley DR, Samanta HK, Lin Z, et al. The terminal (catalytic) adenosine of the HIV LTR controls the kinetics of binding and dissociation of HIV integrase strand transfer inhibitors. Biochemistry, 2008, 47(51): 13481-13488.
- Properties
  - Alternative Name
    
    2-(1,1-dioxothiazinan-2-yl)-N-[(4-fluorophenyl)methyl]-5-hydroxy-1-methyl-6-oxopyrimidine-4-carboxamide
    
    CAS Number
    
    729607-74-3
    
    Molecular Formula
    
    C17H19FN4O5S
    
    Molecular Weight
    
    410.4
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥41 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

BMS-707035

BMS-707035

Background

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