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product name Sabutoclax


Description: Sabutoclax (BI-97C1) is a pan-Bcl-2 inhibitor of Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively. Sabutoclax is a derivative of apogossypolone. It showed a high binding affinity to Bcl-xL both in NMR binding assay and in ITC assay, with a Kd value of 0.11μM. Sabutoclax also showed better cell membrane permeability than other apogossypolone derivatives. In PC3 cells, sabutoclax inhibited cell growth with EC50 value of 0.13 μM. In human BP3 cell line, sabutoclax induced cell apoptosis with IC50 value of 0.049 μM. In mice bearing M2182 cancer xenografts, administration of sabutoclax significantly reduced the tumor size. At dose of 5 mg/kg, sabutoclax induced near complete tumor growth suppression.

References: J Med Chem. 2010 May 27;53(10):4166-76.



Molecular Weight (MW)

700.78
Formula

C42H40N2O8
CAS No.

1228108-65-3
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 100 mg/mL (142.7 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: 54 mg/mL (77 mM)
Solubility (In vivo)

 

other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19400130

General BI-97C1 displays in vivo efficacy in transgenic mice in which Bcl-2 is overexpressed in splenic B-cells and also demonstrates superior single-agent antitumor efficacy in a prostate cancer mouse xenograft model that depends on Mcl-1 for survival
Animal model Bcl-2 transgenic mice, human prostate cancer xenografts
Formulation Ethanol:Cremophor EL:saline = 10:10:80
Dosages 1 , 3, 5 mg/kg
Administration intraperitoneally
Reference [1] Wei J, et al. J Med Chem, 2010, 53(10), 4166-4176

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