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 No. 729607-74-3

Purity & Quality Control

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

BMS-707035 Related Products

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NCT00397566 Withdrawn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 Information & 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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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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