Home Apoptosis Bcl-2 inhibitor Sabutoclax For research use only.

Sabutoclax

Synonyms: BI-97C1

Sabutoclax (BI-97C1) is a pan-Bcl-2 inhibitor, including 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 Chemical Structure

Sabutoclax Chemical Structure

CAS No. 1228108-65-3

Purity & Quality Control

Sabutoclax Related Products

Signaling Pathway

Bcl-2 Signaling Pathways

Bcl-2 Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human H460 cells  Cytotoxic assay 3 days Cytotoxicity against human H460 cells after 3 days by ATP-LITE assay, EC50=0.78 μM 20443627
human PC3 cells Cytotoxic assay 3 days Cytotoxicity against human PC3 cells after 3 days by ATP-LITE assay, EC50=4.64 μM 20443627
MEF  Function assay 30 μM 24 h Induction of apoptosis in MEF expressing wild type Bcl-2 protein at 30 uM after 24 hrs by FITC-conjugated annexin V and propidium iodide staining-based FACS analysis 20443627
BP3 Apoptosis assay 1 to 2 days Induction of apoptosis in human BP3 cells after 1 to 2 days by FITC-conjugated annexin V and propidium iodide staining-based FACS analysis, EC50=0.049μM 20443627
M2182 Antitumor assay 1 to 5 mg/kg Antitumor activity against Mcl-1 overexpressing human M2182 cells xenografted in BALB/c mouse assessed as reduction of tumor size at 1 to 5 mg/kg, ip administered 9 times every 2 days 20443627
M2182 Antitumor assay 5 mg/kg Antitumor activity against Mcl-1 overexpressing human M2182 cells xenografted in BALB/c mouse assessed as complete inhibition of tumor growth at 5 mg/kg, ip administered 9 times every 2 days 20443627
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Biological Activity

Description Sabutoclax (BI-97C1) is a pan-Bcl-2 inhibitor, including 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.
Targets
Mcl-1 [1]
(Cell-free assay)		 Bcl-xL [1]
(Cell-free assay)		 Bcl-2 [1]
(Cell-free assay)		 Bfl-1 [1]
(Cell-free assay)
0.20 μM 0.31 μM 0.32 μM 0.62 μM
In vitro
In vitro

BI-97C1 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, and shows little cytotoxicity against bax-/-bak-/- cells[1]. It is suggest that treatment with the combination regimen of mda-7/IL-24 and BI-97C1 induces autophagy that facilitates apoptosis in association with up-regulation of NOXA, accumulation of Bim, and activation of Bax and Bak[2].
Kinase Assay Competitive fluorescence polarization assays (FPA)
For competitive binding assays, 100 nM GST-Bcl-XL ΔTM protein is preincubated with the tested compound at varying concentrations in 47.5 μL PBS (pH = 7.4) in 96-well black plates at room temperature for 10 min, and then 2.5 μL of 100 nM FITC-labeled Bak BH3 peptide is added to produce a final volume of 50 μL. The wild-type and mutant Bak BH3 peptides are included in each assay plate as positive and negative controls, respectively. After 30 min incubation at room temperature, the polarization values in millipolarization units are measured at excitation/emission wavelengths of 480/535 nm with a multilabel plate reader. IC50 is determined by fitting the experimental data to a sigmoidal dose-response nonlinear regression model. Data reported are mean of three independent experiments. Performance of Bcl-2 and Mcl-1FPA are similar. Briefly, 50 nM of GST-Bcl-2 or -Mcl-1are incubatedwith various concentrations of compound (4 and 11-14) for 2 min, and then 15 nM FITC-conjugated-Bim BH3 peptide is added in PBS buffer. Fluorescence polarization is measured after 10 min.
Cell Research Cell lines PC3, H460, H1299
Concentrations ~1 μM
Incubation Time 72 h
Method

ATP-LITE assay
In Vivo
In vivo

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[1]. Treatment with Ad.5/3-mda-7 and BI-97C1 significantly inhibits the growth of human PC xenografts in nude mice and spontaneously induced PC in Hi-myc transgenic mice. Tumor growth inhibition correlats with increased TUNEL staining and decreased Ki-67 expression in both PC xenografts and prostates of Hi-myc mice[2].
Animal Research Animal Models Bcl-2 transgenic mice, human prostate cancer xenografts
Dosages 1 mg/kg, 3 mg/kg, 5 mg/kg
Administration intraperitoneally

Chemical Information & Solubility

Molecular Weight 700.78 Formula

C42H40N2O8
CAS No. 1228108-65-3 SDF Download Sabutoclax SDF
Smiles CC1=CC2=C(C(=C(C=C2C(=C1C3=C(C4=CC(=C(C(=C4C=C3C)C(=O)NCC(C)C5=CC=CC=C5)O)O)O)O)O)O)C(=O)NCC(C)C6=CC=CC=C6
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (142.69 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 26 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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