Avagacestat (1146699-66-2) Description:
Avagacestat, also known as BMS-708163, is an oral GSI designed for selective inhibition of Aβ synthesis currently in development for the treatment of mild to moderate and predementia AD. In addition to the desired effect on Aβ synthesis, GSIs affect Notch processing, which is thought to mediate some toxic adverse effects reported with this drug class.
Avagacestat (BMS-708163) is a potent γ-secretase inhibitor selective for amyloid precursor protein (APP) over Notch cleavage. Avagacestat inhibits Aβ40 and Aβ42 production with IC50 values of 0.3 nM and 0.27 nM, respectively, compared to IC50 values of 41, 10, 33, and 38 nM respectively for signaling inhibition of the human Notch 1-4 proteins. At higher concentrations BMS-708163 has been found to reverse sensitivity to the EGFR tyrosine kinase inhibitor gefitinib, thought to be by Notch inhibition.
Avagacestat (1146699-66-2) Specifications:
|Synonyms||Avagacestat; BMS708163; BMS-708163; BMS 708163.|
|Purity||>98% (or refer to the Certificate of Analysis)|
|Monoisotopic Mass||520.06 g/mol|
|Color||white to beige|
|Solubility||Soluble in DMSO, not in water|
|Storage Temp.||Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).|
|Shelf life||>5 years if stored properly|
|Handling||Protect from air and light|
|Application||A potent, orally bioavailable inhibitor of γ-secretase|