1146699-66-2 Usage
Description
Avagacestat (BMS-708163) is a small molecule inhibitor that specifically targets the γ-secretase enzyme, which plays a crucial role in the production of amyloid-beta peptides associated with Alzheimer's disease. It has shown potential in modulating embryonic signaling pathways that control stem cell and cellular development processes, making it a promising candidate for cancer therapy as well.
Uses
Used in Pharmaceutical Industry:
Avagacestat (BMS-708163) is used as a γ-secretase inhibitor for the treatment of Alzheimer's disease. By inhibiting the enzyme responsible for the production of amyloid-beta peptides, it aims to slow down the progression of the disease and improve the quality of life for patients.
Used in Cancer Therapy:
Avagacestat (BMS-708163) is used as a therapeutic agent targeting embryonic signaling pathways that control stem cell and cellular development processes in cancer. By modulating these pathways, it may help in the prevention and treatment of various types of cancer, including those that are difficult to treat or have become resistant to conventional therapies.
Biological Activity
bms-708163 is a potent selective and orally bioavailable inhibitor of γ-secretase with ic50 value of 0.3nm [1].the cleavage of amyloid precusor protein app by γ-secretase causes the production of aβ40 and aβ42, which are cytotoxic and cause ad. in vitro assay shows bms-708163 inhibits the formation of aβ40 and aβ42 in h4-8sw cells. it also inhibits the human recombinant cyps in vitro with ic50 value of 20μm. notch receptor is another substrate of γ-secretase. the inhibition of notch signal pathway results in some side effects. it is shown that the activity of bms-708163 to inhibit notch is 190-fold weaker than to app. in female rats, oral administration of bms-708163 significantly reduces the production of aβ in plasma and brain at 10mg/kg and 100mg/kg. in addition, bms-708163 also reduces aβ in brain and csf in male beagle dogs [1].
references
[1] gillman kw, starrett je jr, parker mf, xie k, bronson jj, marcin lr, mcelhone ke, bergstrom cp, mate ra, williams r, meredith je jr, burton cr, barten dm, toyn jh, roberts sb, lentz ka, houston jg, zaczek r, albright cf, decicco cp, macor je, olson re. discovery and evaluation of bms-708163, a potent, selective and orally bioavailable γ-secretase inhibitor. acs med chem lett. 2010 mar 22;1(3):120-4.
Check Digit Verification of cas no
The CAS Registry Mumber 1146699-66-2 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,4,6,6,9 and 9 respectively; the second part has 2 digits, 6 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1146699-66:
(9*1)+(8*1)+(7*4)+(6*6)+(5*6)+(4*9)+(3*9)+(2*6)+(1*6)=192
192 % 10 = 2
So 1146699-66-2 is a valid CAS Registry Number.
1146699-66-2Relevant articles and documents
Synthetic method of inhibitor BMS-708163 produced as beta-amyloid peptide
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, (2018/11/22)
The invention discloses a synthetic process of an anti-HIV virus candidate drug BMS-708163. The process route is novel,the steps are short,the reaction yield is high,the production cost is low,and theprocess has great implementation value and social econo
Novel Alpha-(N-Sulfonamido)Acetamide Compound as an Inhibitor of Beta Amyloid Peptide Production
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Page/Page column 20-21, (2009/05/28)
The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with β-amyloid peptide.
