Avagacestat (BMS-708163) chemical structure
Chemical structureResearch use only
CAT. NO. DC3114Featured

Avagacestat (BMS-708163)

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Product overview

Description & Application

BMS-708163 is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; BMS-708163 also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM.

ParameterValue
Chemical NameAvagacestat
CAS No.1146699-66-2
Synonyms(R)-2-(4-Chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenylsulfonamido)-5,5,5-trifluoropentanamide;BMS-708163;Avagacestat (BMS-708163);(2R)-2-[(4-chlorophenyl)sulfonyl-[[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide;(R)-2-(4-Chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)-phenylsulfonamido)-5,5,5-trifluoropentanamide;(R)-2-[[4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide;Avagacestat;BMS-708163 (avagacestat);Pentanamide, 2-[[(4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoro-, (2R)-;BMS708163;(2R)-2-[N-[(4-Chlorophenyl)sulfonyl]-N-[[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide;(2R)-2-[N-[(4-Chlorophenyl)sulfonyl]-N-[2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl]amino]-5,5,5-trifluoropentanamide;BMS 708163;TQ44WWY45Q;(2R)-2-[(4-Chlorophenyl)sulfonyl-[[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoro-pentanamide;(2R)-5,5,5-trifluoro-2-(N-;(2R)-5,5,5-trifluoro-2-(N-{[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl}4-chlorobenzenesulfonamido)pentanamide;(2R)-2-[(4-Chlorophenyl)sulfo;BMS-708163-01;EX-A2871;BDBM50458169;D09869;(2R)-2-[(4-chlorophenyl)sulonyl-[[2-luoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-triluoropentanamide;AKOS005146523;MFCD13195458;(R)-2-((4-Chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenyl)sulfonamido)-5,5,5-trifluoropentanamide;PENTANAMIDE, 2-(((4-CHLOROPHENYL)SULFONYL)((2-FLUORO-4-(1,2,4-OXADIAZOL-3-YL)PHENYL)METHYL)AMINO)-5,5,5-TRIFLUORO-, (2R)-;BCPP000327;HMS3884O07;SW218162-2;C71464;DB11893;1146699-66-2;UNII-TQ44WWY45Q;AKOS016016280;s1262;CHEMBL1090771;CCG-269860;(2R)-2-[[(4-Chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoro-pentanamide;BCP9000429;AVAGACESTAT [WHO-DD];SCHEMBL310019;Avagacestat; BMS-708163;CHEBI:177493;Avagacestat (USAN);(2R)-2-[[(4-Chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide;BCP01770;GTPL6489;(2R)-2-[(4-chlorophenyl)sulfonyl-[[2-fluoranyl-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-tris(fluoranyl)pentanamide;MRF-0000009;DTXSID40150811;Avagacestat [USAN];MLS006011074;A894166;Avagacestat, >=98% (HPLC);NSC-761217;SMR004676648;HY-50845;EN9;AVAGACESTAT [INN];AS-75078;BMS-708163;(R)-2-(4-chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenylsulfonamido)-5,5,5-trifluoropentanamide;Avagacestat [USAN:INN];BMS-70816301;NCGC00346504-01;NS00072555;Q27074630;(2R)-2-(N-((4-Chlorophenyl)sulfonyl)-N-((2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl)methyl)amino)-5,5,5-trifluoropentanamide;BCP0726000124;CS-0180;NSC761217;(2R)-5,5,5-trifluoro-2-(N-((2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl)methyl)4-chlorobenzenesulfonamido)pentanamide;BRD-K83720053-001-03-8;N~2~-[(4-chlorophenyl)sulfonyl]-5,5,...
FormulaC20H17ClF4N4O4S
M.Wt520.884996175766
SMILESClC1C=CC(=CC=1)S(N(CC1C=CC(C2=NOC=N2)=CC=1F)[C@@H](C(N)=O)CCC(F)(F)F)(=O)=O
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

BMS-708163 is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; BMS-708163 also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM.

In Vitro

IC50: 0.27 nM (γ-secretase, Aβ42), 0.30 nM (γ-secretase, Aβ40), 20 μM (CYP2C19)[1], 0.84 nM (NICD)[2]

In Vivo

BMS-708163 significantly reduces both plasma and brain Aβ40 levels relative to control at 10 and 100 mg/kg for the entire dosing interval, demonstrates significant Aβ40 lowering for 8 h after an oral dose of 1 mg/kg, and significantly lowers CSF Aβ40 levels in rats, when measured 5 h after single oral doses ranging from 3 to 100 mg/kg[1]. BMS-708163 (10 mg/kg) monotherapy has a minor inhibitory effect on PC9/AB2 tumor growth compared with gefitinib alone. BMS-708163 monotherapy results in a slight increase in caspase 3 expression as well as a mild decrease in Ki-67 expression in vivo. In the xenograft lung cancer samples treated with BMS-708163 plus gefitinib, there are a marked increase in caspase 3 expression and a reduction in Ki-67 staining[3].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

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Refer to the certificate supplied with your lot for batch-specific release results.

Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Solution calculator

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