Fostemsavir (BMS663068)

InvivoChem Cat #:V3501CAS #:864953-29-7Purity >=98%

Description: Fostemsavir (BMS-663068) is the phosphonooxymethyl prodrug of BMS-626529 which is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells. The activity of BMS-626529 is virus dependent, due to heterogeneity within gp120. In order to better understand the anti-HIV-1 spectrum of BMS-626529 against HIV-1, in vitro activities against a wide variety of laboratory strains and clinical isolates were determined. BMS-626529 had half-maximal effective concentration (EC(50)) values of< 10 nm='' against='' the='' vast='' majority='' of='' viral='' susceptibility='' varied='' by=''> 6 log(10), with half-maximal effective concentration values in the low pM range against the most susceptible viruses. The in vitro antiviral activity of BMS-626529 was generally not associated with either tropism or subtype, with few exceptions. Measurement of the binding affinity of BMS-626529 for purified gp120 suggests that a contributory factor to its inhibitory potency may be a relatively long dissociative half-life. Finally, in two-drug combination studies, BMS-626529 demonstrated additive or synergistic interactions with antiretroviral drugs of different mechanistic classes. These results suggest that BMS-626529 should be active against the majority of HIV-1 viruses and support the continued clinical development of the compound.

References: Antimicrob Agents Chemother. 2012 Jul; 56(7):3498-507.

Related CAS#: 864953-29-7(free base) 864953-39-9 (Fostemsavir Tris)

864953-29-7(

-20C for 3 years in powder form

Synonym: BMS-663068; BMS663068; BMS-663068 dihydrate; BMS 663068; Fostemsavir
Chemical Name: (3-(2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl)-4-methoxy-7-(3-methyl-1H-1, 2, 4-triazol-1-yl)-1H-pyrrolo[2, 3-c]pyridin-1-yl)methyl dihydrogen phosphate
InChi Key: SWMDAPWAQQTBOG-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H26N7O8P/c1-16-27-14-32(28-16)23-21-20(19(39-2)12-26-23)18(13-31(21)15-40-41(36, 37)38)22(33)25(35)30-10-8-29(9-11-30)24(34)17-6-4-3-5-7-17/h3-7, 12-14H, 8-11, 15H2, 1-2H3, (H2, 36, 37, 38)
SMILES Code: CC1=NN(C=N1)C2=NC=C(C3=C2N(C=C3C(=O)C(=O)N4CCN(CC4)C(=O)C5=CC=CC=C5)COP(=O)(O)O)OC