BM0005

Avagacestat

≥98% (HPLC)

• Synonyme(s) : (2R)-2-[N-[(4-Chlorophenyl)sulfonyl]-N-[[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide, (R)-2-(4-Chloro-N-(2-fluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)phenylsulfonamido)-5,5,5-trifluoropentanamide, BMS-708163
• Formule empirique (notation de Hill): C₂₀H₁₇ClF₄N₄O₄S
• Numéro CAS: 1146699-66-2
• Poids moléculaire : 520.88
• Numéro MDL: MFCD13195458
• Code UNSPSC : 12352200
• ID de substance PubChem : 329774352

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: powder
• Couleur: white to beige
• Solubilité: DMSO: 30 mg/mL, clear
• Température de stockage: room temp
• Chaîne SMILES: NC([C@@H](CCC(F)(F)F)N(S(C1=CC=C(Cl)C=C1)(=O)=O)CC2=C(F)C=C(C3=NOC=N3)C=C2)=O
• InChI: 1S/C20H17ClF4N4O4S/c21-14-3-5-15(6-4-14)34(31,32)29(17(18(26)30)7-8-20(23,24)25)10-13-2-1-12(9-16(13)22)19-27-11-33-28-19/h1-6,9,11,17H,7-8,10H2,(H2,26,30)/t17-/m1/s1
• Clé InChI: XEAOPVUAMONVLA-QGZVFWFLSA-N
• Informations sur le gène: human ... APH1A(51107) , APH1B(83464) , NCSTN(23385) , PSEN1(5663) , PSEN2(5664) , PSENEN(55851)

Description

Actions biochimiques/physiologiques

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.

Caractéristiques et avantages

Avagacestat is available through a partnership with Bristol-Myers Squibb (BMS). To learn more and view other BMS compounds, visit sigma.com/BMS.

Informations légales

Sold for research purposes only under agreement from BMS.

Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H315,H319,H335
• Conseils de prudence: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• Classification des risques: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• Organes cibles: Respiratory system
• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable