Home Microbiology Integrase inhibitor BMS-707035 For research use only.

BMS-707035

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

BMS-707035 Chemical Structure

BMS-707035 Chemical Structure

CAS: 729607-74-3

Selleck's BMS-707035 has been cited by 1 publication

Purity & Quality Control

Batch: S136601 DMSO] 38 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.8%
99.8

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Biological Activity

Description BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.
Targets
HIV-I integrase [1]
15 nM
In vitro
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00397566 Withdrawn HIV Infections Bristol-Myers Squibb February 2007 Phase 2

Chemical lnformation & Solubility

Molecular Weight 410.42 Formula

C17H19FN4O5S
CAS No. 729607-74-3 SDF Download BMS-707035 SDF
Smiles CN1C(=O)C(=C(N=C1N2CCCCS2(=O)=O)C(=O)NCC3=CC=C(C=C3)F)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 38 mg/mL ( (92.58 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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