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Key Documents

SML3695

Sabutoclax

new

≥98% (HPLC)

Synonym(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

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About This Item

Empirical Formula (Hill Notation):
C42H40N2O8
CAS Number:
Molecular Weight:
700.78
UNSPSC Code:
12352200

Quality Level

Assay

≥98% (HPLC)

form

powder

color

white to beige

shipped in

wet ice

storage temp.

-10 to -25°C

Biochem/physiol Actions

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).

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