Name | Sabutoclax |
Synonyms | BI-97C1 SABUTOCLAX Sabutoclax (1R)-1,1',6,6',7,7'-Hexahydroxy-3,3'-dimethyl-N5,N5'-bis[(2R)-2-phenylpropyl]-[2,2'-binaphthalene]-5,5'-dicarboxamide [2,2'-Binaphthalene]-5,5'-dicarboxamide, 1,1',6,6',7,7'-hexahydroxy-3,3'-dimethyl-N5,N5'-bis[(2R)-2-phenylpropyl]-, (1R) |
CAS | 1228108-65-3 |
Molecular Formula | C42H40N2O8 |
Molar Mass | 700.78 |
Density | 1.358±0.06 g/cm3(Predicted) |
Melting Point | >130°C (dec.) |
Boling Point | 905.9±65.0 °C(Predicted) |
Solubility | DMSO (Slightly), Ethyl Acetate (Slightly), Methanol (Slightly) |
Appearance | Solid |
Color | Light Brown to Brown |
pKa | 7.35±0.50(Predicted) |
Storage Condition | -20°C Freezer |
In vitro study | BI-97C1 effectively inhibit the growth of human prostate cancer, lung cancer, and lymphoma cell lines with EC50 values of 0.13, 0.56, and 0.049 μm, respectively, using a combination of mda-7/IL-24 and BI-97C1 for bax, it can induce autophagy, which is beneficial to cell apoptosis, correspondingly upregulate NOXA, make Bim accumulate, and activate Bax and Bak. |
In vivo study | BI-97C1 effectively acts on transgenic mice with spleen B cells overexpressing Bcl-2, and has a strong anti-tumor effect on the transplanted tumor model of prostate cancer mice. Ad.5/3-mda-7 and BI-97C1 treatment of nude mice and Hi-myc transgenic mice significantly inhibited the growth of human PC xenografts and spontaneously induced PC. Treatment of PC xenografts and the prostate of Hi-myc mice inhibited tumor growth and was associated with increased TUNEL staining and decreased Ki-67 expression. |
biological activity | Sabutoclax is a pan-Bcl-2 inhibitor that acts on Bcl-xL, Bcl-2, Mcl-1 and Bfl-1, the IC50 values were 0.31 μm, 0.32 μm, 0.20 μm and 0.62 μm, respectively. Sabutoclax (BI-97C1) is a pan-Bcl-2 inhibitor acting on Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μm, 0.32 μm, 0.20 M and 0.62 M. |
Target | Value |
Mcl-1 (Cell-free assay) | 0.20 μM |
Bcl-xL (Cell-free assay) | 0.31 μM |
Bcl-2 (Cell-free assay) | 0.32 μM |
Bfl-1 (Cell-free assay) | 0.62 μM |