BMS-707035 - 10mM in DMSO , Integrase inhibitor, CAS No.729607-74-3, Integrase inhibitor

CAS: 729607-74-3 Cat. No.: B408592 Molecular Weight: 410.42

GRADE & PURITY 10mM in DMSO

Synonyms

4-Pyrimidinecarboxamide, N-[(4-fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-6-oxo-2-(tetrahydro-1,1-dioxido-2H-1,2-thiazin

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

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

In vivo

Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

4-Pyrimidinecarboxamide, N-[(4-fluorophenyl)methyl]-1, 6-dihydro-5-hydroxy-1-methyl-6-oxo-2-(tetrahydro-1, 1-dioxido-2H-1, 2-thiazin

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Mechanism of action

Integrase inhibitor

Product Properties

• ALogP: 1

Names and Identifiers

• Isomeric SMILES: CN1C(=O)C(=C(N=C1N2CCCCS2(=O)=O)C(=O)NCC3=CC=C(C=C3)F)O
• Molecular Weight: 410.42
• Reaxy-Rn: 15489912
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=15489912&ln=