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Sabutoclax

Name: Sabutoclax
Brand: Selleck Chemicals
SKU: S8061
Rating: 5 (10 reviews)

Synonyms: BI-97C1

Catalog No.S8061 Purity:99.51%

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

CAS No. 1228108-65-3

Purity & Quality Control

Batch: Purity: 99.51%

99.51

Sabutoclax Related Products

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Signaling Pathway

Bcl-2 Signaling Pathway

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

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)
Kinase Assay	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

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5% DMSO 1 95% corn oil	0.5mg/ml (0.71mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml (7.13mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil	0.5mg/ml (0.71mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml (7.13mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
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