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BMS-707035

Catalog No. T6420   CAS 729607-74-3

BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.

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BMS-707035 Chemical Structure
BMS-707035, CAS 729607-74-3
Pack Size Availability Price/USD Quantity
2 mg In stock $ 34.00
5 mg In stock $ 55.00
10 mg In stock $ 98.00
25 mg In stock $ 197.00
50 mg In stock $ 360.00
100 mg In stock $ 587.00
1 mL * 10 mM (in DMSO) In stock $ 61.00
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Purity: 99.83%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.
Targets&IC50 HIV-I integrase:15 nM
In vitro BMS-707035 is a pyrimidine carboxamide similar to Raltegravir, the first integrase inhibitor licensed for clinical use. BMS-707035 is a potent, specific, and reversible HIV-I integrase (IN) inhibitor that blocks HIV IN strand transfer activity with IC50 of 15 nM. [1] However, several IN mutations, including V75I, Q148R, V151I, and G163R are found to confer resistance to HIV IN inhibitors. The binding of BMS-707035 and target DNA to IN are mutually exclusive events, as revealed by the fact that the inhibition of strand transfer catalysis by BMS-707035 is overcome by increasing amount of target DNA. The binding affinity of BMS-707035 to IN is also affected by the four terminal bases at the 5' end of the pre-processed U5 long terminal repeat (LTR). Gln148 of IN is crucial for the binding of BMS-707035 to IN. [1] The 3' terminus of the viral LTR, on the other hand, retards the rate of BMS-707035 association with IN, by regulating the kinetics of binding and dissociation. [2]
Molecular Weight 410.42
Formula C17H19FN4O5S
CAS No. 729607-74-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 36 mg/mL (87.7 mM)

TargetMolReferences and Literature

1. Dicker IB, et al. J Biol Chem, 2007, 282(43), 31186-31196. 2. Langley DR, et al. Biochemistry, 2008, 47(51), 13481-13488.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Immunology/Inflammation Compound Library NO PAINS Compound Library Bioactive Compound Library ReFRAME Related Library Bioactive Compounds Library Max Anti-Viral Compound Library Preclinical Compound Library Target-Focused Phenotypic Screening Library PPI Inhibitor Library

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Keywords

BMS-707035 729607-74-3 Microbiology/Virology Proteases/Proteasome HIV Protease HIV-1 integrase strand transfer HIV Human immunodeficiency virus antiviral phamacokinetics HIV Integrase BMS 707035 CYP inhibit strand transfer Inhibitor BMS707035 inhibitor

 

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