Home Proteases Secretase inhibitor - Beta Amyloid inhibitor - Notch inhibitor Avagacestat (BMS-708163) For research use only.

Avagacestat (BMS-708163)

Avagacestat (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2.

Avagacestat (BMS-708163) Chemical Structure

Avagacestat (BMS-708163) Chemical Structure

CAS: 1146699-66-2

Selleck's Avagacestat (BMS-708163) has been cited by 22 Publications

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Purity & Quality Control

Batch: Purity: 99.63%
99.63

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human IMR32 cell Function assay 2 h Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA, IC50=0.13 nM 23312944
human H4 cells Function assay Inhibition of gamma secretase-mediated amyloid beta42 production in human H4 cells expressing human APP swedish mutant, IC50=0.225 μM 22420884
HEK293 cells Function assay Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis, IC50=1.2 nM 23312944
CHO cells Function assay Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA, ED50=1.2 nM 23713656
human IMR32 cell Function assay 2 h Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA, IC50=1.5 nM 23312944
human 786-0 cell Growth inhibition assay Inhibition of human 786-0 cell growth in a cell viability assay, IC50=0.32173 μM SANGER
human NCI-H810 cell Growth inhibition assay Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50=0.42598 μM SANGER
human IGR-1 cell Growth inhibition assay Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=1.04778 μM SANGER
human SK-MEL-3 cell Growth inhibition assay Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=1.49922 μM SANGER
human HT-1080 cell Growth inhibition assay Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=2.48764 μM SANGER
human NCI-H23 cell Growth inhibition assay Inhibition of human NCI-H23 cell growth in a cell viability assay, IC50=3.9322 μM SANGER
human Calu-6 cell Growth inhibition assay Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=4.96014 μM SANGER
human CAPAN-1 cell Growth inhibition assay Inhibition of human CAPAN-1 cell growth in a cell viability assay, IC50=5.17886 μM SANGER
human COLO-668 cell Growth inhibition assay Inhibition of human COLO-668 cell growth in a cell viability assay, IC50=5.40221 μM SANGER
human TE-6 cell Growth inhibition assay Inhibition of human TE-6 cell growth in a cell viability assay, IC50=6.19082 μM SANGER
human LCLC-97TM1 cell Growth inhibition assay Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=10.0886 μM SANGER
human CAS-1 cell Growth inhibition assay Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=13.671 μM SANGER
human RPMI-2650 cell Growth inhibition assay Inhibition of human RPMI-2650 cell growth in a cell viability assay, IC50=13.8124 μM SANGER
human MDA-MB-157 cell Growth inhibition assay Inhibition of human MDA-MB-157 cell growth in a cell viability assay, IC50=14.2431 μM SANGER
human KINGS-1 cell Growth inhibition assay Inhibition of human KINGS-1 cell growth in a cell viability assay, IC50=14.3762 μM SANGER
human BB49-HNC cell Growth inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=14.4138 μM SANGER
human SK-UT-1 cell Growth inhibition assay Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=14.6882 μM SANGER
human EW-11 cell Growth inhibition assay Inhibition of human EW-11 cell growth in a cell viability assay, IC50=14.8832 μM SANGER
human D-502MG cell Growth inhibition assay Inhibition of human D-502MG cell growth in a cell viability assay, IC50=14.9034 μM SANGER
human MMAC-SF cell Growth inhibition assay Inhibition of human MMAC-SF cell growth in a cell viability assay, IC50=15.0833 μM SANGER
human NCI-H1648 cell Growth inhibition assay Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=15.778 μM SANGER
human NCI-H292 cell Growth inhibition assay Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50=15.8806 μM SANGER
human NMC-G1 cell Growth inhibition assay Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=16.6293 μM SANGER
human SAS cell Growth inhibition assay Inhibition of human SAS cell growth in a cell viability assay, IC50=17.7812 μM SANGER
human HCT-116 cell Growth inhibition assay Inhibition of human HCT-116 cell growth in a cell viability assay, IC50=18.7965 μM SANGER
human SBC-5 cell Growth inhibition assay Inhibition of human SBC-5 cell growth in a cell viability assay, IC50=19.03 μM SANGER
Click to View More Cell Line Experimental Data

Biological Activity

Description Avagacestat (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2.
Features Appears to be more “notch sparing” than semagacestat (LY450139).
Targets
Aβ42 [1]
(in H4-8Sw cells)		 Aβ40 [1]
(in H4-8Sw cells)
0.27 nM 0.3 nM
In vitro
In vitro BMS-708163 exhibits weaker selectivity for inhibition of Notch processing with 193-fold IC50 value. [1]
In Vivo
In vivo Oral administration of BMS-708163 significantly reduces Aβ40 levels for sustained periods in brain, plasma, and cerebrospinal fluid in rats and dogs. BMS-708163 has no dose-limiting effects in dogs (3 mg/kg during 6 months), with a high brain to plasma ratio (2.4). [1]
Animal Research Animal Models Female Harlan Sprague-Dawley rats or ATM-405-142K9 with 7- 10 month old Na?ve, grade II beagles
Dosages 10 mg/kg (rats) or 2.5 mg/kg (dogs)
Administration Dosed daily by oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01002079 Completed Alzheimer Disease Bristol-Myers Squibb|PRA Health Sciences August 2010 Phase 1
NCT01057030 Completed Alzheimer Disease Bristol-Myers Squibb March 2010 Phase 1
NCT01042314 Completed Alzheimer Disease Bristol-Myers Squibb January 2010 Phase 1
NCT01039194 Completed Alzheimer Disease Bristol-Myers Squibb January 2010 Phase 1
NCT00979316 Completed Alzheimer Disease Bristol-Myers Squibb September 2009 Phase 1
NCT00890890 Terminated Alzheimer''s Disease Bristol-Myers Squibb May 2009 Phase 2

Chemical lnformation & Solubility

Molecular Weight 520.88 Formula

C20H17ClF4N4O4S
CAS No. 1146699-66-2 SDF Download Avagacestat (BMS-708163) SDF
Smiles C1=CC(=CC=C1S(=O)(=O)N(CC2=C(C=C(C=C2)C3=NOC=N3)F)C(CCC(F)(F)F)C(=O)N)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 104 mg/mL ( (199.66 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

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