| Name | Avagacestat |
| Description | Avagacestat (BMS-708163) (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. |
| Cell Research | BMS-708163 is dissolved in DMSO. The cell viability is assessed using a tetrazolium salt (WST-8)-based colorimetric assay from the Cell Counting Kit 8 (CCK-8). The cells are seeded into 96-well plates at an initial density of 5×103 cells/well and cultured for 24?h, after which the cells are cultured with DMSO, increased concentrations of gefitinib or BMS708163, BIBW2992, or the combination of BMS708163 and BIBW2992 for an additional 48?h. The A450 is measured in a microplate reader after 10?μL of CCK-8 solution is added and incubated for 1?h. The percentage of growth is shown relative to untreated controls. |
| In vitro | BMS-708163 exhibits weaker selectivity for inhibition of Notch processing with 193-fold IC50 value. [1] |
| 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+90% Corn Oil : 4 mg/mL (7.68 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 96 mg/mL (184.3 mM), Sonication is recommended.
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| Keywords | γ-secretase | γ secretase(Aβ42) | γ secretase(Aβ40) | Notch | Inhibitor | inhibit | Gammasecretase | Gamma secretase | BMS708163 | BMS 708163 | Avagacestat |
| Inhibitors Related | Valproic acid sodium salt | Aβ42-IN-2 | Sulindac sulfide | Tangeretin | gamma-secretase modulator 1 | Valproic Acid | Nirogacestat | Hexamethylene bisacetamide | CB-103 | Prednisone acetate | Carvacrol | RO7185876 |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | HIF-1 Signaling Pathway Compound Library | Hematonosis Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Human Metabolite Library | Anti-Cancer Drug Library | Neuronal Differentiation Compound Library |
United States
