Molecular Weight(MW): 520.88
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.
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A panel of GICs lines was treated with various concentrations of γ secretase inhibitors BMS-708163. Cells were treated with increasing concentrations of γ secretase inhibitors in triplicate wells for 72 hours, and cell viability was assessed by CellTiter-Blue assay as described in Materials and Methods. The results shown are of a single experiment with three independent replicates cell viability was measured by CellTiter-Blue assay. The graph depicts cell viability at 72 hours. Cell viability in the vehicle control was considered as to be 100%.
Stem Cells 2014 32(1), 301-12. Avagacestat (BMS-708163) purchased from Selleck.
Nuclear targeting of anMan-containing HS degradation products is suppressed by β-secretase inhibition in WT and Tg2576 MEFs and by γ-secretase inhibition in WT but not in Tg2576 MEFs. A-H, representative immunofluorescence images of wild-type MEF cells (A-D) and Tg2576 cells (E-H) treated with 100 nm β-inhibitor (A, B, E, and F) or 10 nM BMS-708163 (C, D, G, and H) for 48 h followed by treatment with 1 mm ascorbate for 1 h (B, D, F, and H) and then stained with DAPI and mAb AM. Bar, 20 um. Tg2576, MEFs from AD mouse model; DAPI, nuclear stain; Asc, ascorbate. These experiments were repeated twice.
J Biol Chem 2014 289(30), 20871-8. Avagacestat (BMS-708163) purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|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).|
BMS-708163 exhibits weaker selectivity for inhibition of Notch processing with 193-fold IC50 value. 
|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). |
|In vitro||DMSO||104 mg/mL (199.66 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01002079||Completed||Alzheimer Disease||Bristol-Myers Squibb|PRA Health Sciences||August 2010||Phase 1|
|NCT01079819||Completed||Alzheimers Disease||Bristol-Myers Squibb||April 2010||Phase 1|
|NCT01057030||Completed||Alzheimer Disease||Bristol-Myers Squibb||March 2010||Phase 1|
|NCT01039194||Completed||Alzheimer Disease||Bristol-Myers Squibb||January 2010||Phase 1|
|NCT01042314||Completed||Alzheimer Disease||Bristol-Myers Squibb||January 2010||Phase 1|
|NCT00979316||Completed||Alzheimer Disease||Bristol-Myers Squibb||September 2009||Phase 1|
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.
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