Comparison

Avagacestat European Partner

Item no. HY-50845-100mg
Manufacturer MedChem Express
CASRN 1146699-66-2
Amount 100 mg
Quantity options 100 mg 10 mM/1 mL 10 mg 1 mg 25 mg 50 mg 5 mg
Category
Type Inhibitors
Specific against other
Purity 99.92
Citations [1]Gillman KW, et al. Letter Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor. Med Chem Lett, 2010, 1 (3), 120-124.|[2]Crump CJ, et al. BMS-708,163 targets presenilin and lacks notch-sparing activity. Biochemistry. 2012 Sep 18;51(37):7209-11.|[3]Xie M, et al. γ Secretase inhibitor BMS-708163 reverses resistance to EGFR inhibitor via the PI3K/Akt pathway in lung cancer. J Cell Biochem. 2015 Jun;116(6):1019-27.|[4]Borghys H, et al. A canine model to evaluate efficacy and safety of γ-secretase inhibitors and modulators. J Alzheimers Dis. 2012;28(4):809-22.|[5]Vladimir Coric, et al. Safety and tolerability of the γ-secretase inhibitor avagacestat in a phase 2 study of mild to moderate Alzheimer disease. Arch Neurol. 2012 Nov;69(11):1430-40.
Smiles O=S(N([C@@H](C(N)=O)CCC(F)(F)F)CC1=CC=C(C2=NOC=N2)C=C1F)(C3=CC=C(Cl)C=C3)=O
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Alias BMS-708163
Shipping Condition Room temperature
Available
Manufacturer - Type
Reference compound
Manufacturer - Applications
Cancer-programmed cell death
Manufacturer - Targets
Notch; γ-secretase
Shipping Temperature
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Molecular Weight
520.89
Product Description
Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM. Avagacestat can be used for Alzheimer disease research.
Manufacturer - Research Area
Cancer
Solubility
DMSO: ≥ 100 mg/mL
Manufacturer - Pathway
Neuronal Signaling; Stem Cell/Wnt
Clinical information
Phase 2

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 100 mg
Available: In stock
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