GLPBio

BMS-707035

Catalog No.: GC11923Purity:>99.50%
COASDSData Sheet

Les produits sont exclusivement destinés à la recherche. Ils ne doivent pas être utilisés chez l’être humain. Nous ne vendons pas aux patients.

BMS-707035
Cas No.: 729607-74-3
10mM (in 1mL DMSO)In Stock
$48.00
1
1mgIn Stock
$32.00
1
5mgIn Stock
$53.00
1
10mgIn Stock
$86.00
1
25mgIn Stock
$171.00
1
50mgIn Stock
$288.00
1
100mgIn Stock
$405.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citations

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    Nature
    641, 529–536 (2025)
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    Nature
    628, 630–638 (2024)
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    Nature
    632, 686–694 (2024)
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    Nature
    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
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    Science
    387(6739) (2025)
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    Science
    387(6734) (2025)
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    Cell Research
    35, 97–116 (2025)
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    34, 683–706 (2024)
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    33, 273–287 (2023)
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    33, 546–561 (2023)
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    33, 904–922 (2023)
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    31, 1291–1307 (2021)

Description

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].
References:
[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.

Protocole (Protocol)

Cell experiment [1]:

Cell lines

Human immunodeficiency virus (HIV)

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

IC50: 15 nM

Applications

BMS-707035 was a potent, specific, and reversible HIV-I integrase (IN) inhibitor that blocked HIV IN strand transfer activity with IC50 of 15 nM. Several IN mutations, including V75I, Q148R, V151I, and G163R were resistant to HIV IN inhibitors. The binding of BMS-707035 and target DNA to IN was mutually exclusive events, as revealed by the fact that the inhibition of strand transfer catalysis by BMS-707035 was overcome by increasing amount of target DNA. The binding affinity of BMS-707035 to IN was affected by the four terminal bases at the 5' end of the pre-processed U5 long terminal repeat (LTR). Gln148 of IN was crucial for the binding of BMS-707035 to IN.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Dicker I B, Samanta H K, Li Z, et al. Changes to the HIV long terminal repeat and to HIV integrase differentially impact HIV integrase assembly, activity, and the binding of strand transfer inhibitors[J]. Journal of Biological Chemistry, 2007, 282(43): 31186-31196.

Documents produit (Product Documents)

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Propriétés chimiques (Chemical Properties)

N° CAS
729607-74-3
Nom chimique
2-(1,1-dioxothiazinan-2-yl)-N-[(4-fluorophenyl)methyl]-5-hydroxy-1-methyl-6-oxopyrimidine-4-carboxamide
SMILES
CN1C(=O)C(=C(N=C1N2CCCCS2(=O)=O)C(=O)NCC3=CC=C(C=C3)F)O
Formule moléculaire
C17H19FN4O5S
Masse moléculaire
410.4
Solubilité
≥ 41 mg/mL in DMSO
Conservation
Store at -20°C
Conseils généraux
Choisissez un solvant adapté selon les données de solubilité du produit. Après préparation, répartissez la solution mère en aliquotes afin d’éviter les cycles répétés de congélation-décongélation.
Utilisez les solutions mères dans les 6 mois si elles sont conservées à -80°C, ou dans le mois si elles sont conservées à -20°C.
Pour améliorer la solubilité, réchauffez le tube à 37°C et soniquez-le pendant une durée appropriée.
Conditions d’expédition
Les échantillons d’évaluation sont expédiés avec des blocs réfrigérants. Les autres formats sont expédiés à température ambiante ou, sur demande, avec des blocs réfrigérants.

Calculateurs (Calculators)Molarité / Dilution / Masse moléculaire / Conversion d’unités / Formulation in vivo / Solubilité

g/mol

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