Sabutoclax Inhibitor CAS No. 1228108-65-3

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Chemical Characteristic

Product Name	Sabutoclax
Synonyms	BI-97C1
CAS No.	1228108-65-3
Molecular Weight	700.78
Formula	C₄₂H₄₀N₂O₈
Chemical Name	(1R)-1,1',6,6',7,7'-Hexahydroxy-3,3'-dimethyl-N5,N5'-bis[(2R)-2-phenylpropyl]-[2,2'-binaphthalene]-5,5'-dicarboxamide
Smiles	c1(c(c(cc2c(c(c(cc12)O)O)C(=O)NC[C@H](C)c1ccccc1)C)c1c(c2c(cc1C)c(c(c(c2)O)O)C(=O)NC[C@H](C)c1ccccc1)O)O
Chemical Structure

Biological activities

Sabutoclax is a novel and potent Bcl-2 anti-apoptotic proteins inhibitor. Sabutoclax inhibits the binding of BH3 peptides to Bcl-X_{L, Bcl-2, Mcl-1 and Bfl-1 with IC50 values of 0.31, 0.32, 0.20 and 0.62 μM, respectively. Sabutoclax also potently inhibits cell growth of human prostate cancer, lung cancer and lymphoma cell lines with EC50 values of 0.13, 0.56 and 0.049 μM, respectively. However, sabutoclax shows little cytotoxicity against bax^−/−bak^−/−cells.^[1] In vitro, sabutoclax also inhibits blast crisis leukemia stem cells (BC LSC) survival. Sabutoclax sensitizes marrow-niche-engrafted BC LSCs to dasatinib.^[2] Sabutoclax sensitizes prostate tumors to mda-7/IL-24-induced apoptosis. In vivo, treatment with Ad.5/3-mda-7 and Sabutoclax significantly inhibits the growth of human prostate cancer xenografts in nude mice and spontaneously induced PC in Hi-myc transgenic mice.^[3] In the human prostate cancer xenografts in athymic nude mice, sabutoclax treatment (5 mg/kg) induces near complete inhibition of tumor growth compared with the control groups. Sabutoclax (3 mg/kg) inhibits tumor growth to ~60% of the tumor volume in the control group.^[1]}

Protocols

In vivo: Sabutoclax is dissolved in ethanol/Cremophor EL/saline (10:10:80).^[3]

References

[1] Wei J, et al. BI-97C1, an optically pure Apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. J Med Chem. 2010, 53(10): 4166-4176. [2] Goff DJ, et al. A Pan-BCL2 inhibitor renders bone-marrow-resident human leukemia stem cells sensitive to tyrosine kinase inhibition. Cell Stem Cell. 2013, 12(3): 316-328. [3] Dash R, et al. Apogossypol derivative BI-97C1 (Sabutoclax) targeting Mcl-1 sensitizes prostate cancer cells to mda-7/IL-24-mediated toxicity. Proc Natl Acad Sci U S A. 2011, 108(21): 8785-8790.

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