SML3695

Sabutoclax

≥98% (HPLC)

• Synonyme(s) : (1R)-1,1′,6,6′,7,7′-Hexahydroxy-3,3′-dimethyl-N5,N5′-bis[(2R)-2-phenylpropyl]-[2,2′-binaphthalene]-5,5′-dicarboxamide, (RS)-1,1′,6,6′,7,7′-Hexahydroxy-3,3′-dimethyl-N5-((R)-2-phenylpropyl)-N5′-((R)-2-phenylpropyl)-2,2′-binaphthyl-5,5′-dicarboxamide, BI-97C1, BI97C1
• Formule empirique (notation de Hill): C₄₂H₄₀N₂O₈
• Numéro CAS: 1354327-17-5
• Poids moléculaire : 700.78
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: powder
• Couleur: white to beige
• Conditions d'expédition: wet ice
• Température de stockage: -10 to -25°C

Description

Actions biochimiques/physiologiques

Potent inhibitor against antiapoptotic Bcl-2 family proteins (Bcl-xL, Bcl-2, Mcl-1, Bfl-1) with anti-cancer efficacy in cultures and in vivo.



Sabutoclax (BI-97C1) is a potent inhibitor against antiapoptotic Bcl-2 family proteins (IC50 in nM against BH3 peptide binding = 310/Bcl-xL, 320/Bcl-2, 200/Mcl-1, 620/Bfl-1) that induces apoptosis in cancer cultures (EC50 in nM = 49/BP3, 130/PC3, 420/H460) with little cytotoxicity against bax-/-bak-/- cells. Sabutoclax anti-tumore efficacy in vivo, including a Bcl-2 transgenic model (42 mg/kg i.p. in mice expressing human Bcl-2 in splenic B-cells) and a M2182 prostate cancer xenograft model (1,3, 5 mg/kg q.o.d. i.p. in mice).