Sabutoclax

Catalog No.S8061 Synonyms: BI-97C1

For research use only.

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

Selleck's Sabutoclax has been cited by 7 Publications

2 Customer Reviews

Purity & Quality Control

Choose Selective Bcl-2 Inhibitors

Other Bcl-2 Products

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

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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human H460 cells  NGfLZ2NEgXSxdH;4bYPDqGG|c3H5 NGfXUWU{KGSjeYO= NWjMVlVXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUDR4MDDj[YxteyCjZoTldkA{KGSjeYOgZpkhSVSSLVzJWGUh[XO|YYmsJGVEPTB;MD63PEDPxE1? MljBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB2NEO2NlcoRjJyNESzOlI4RC:jPh?=
human PC3 cells M3r4WWN6fG:2b4jpZ:Kh[XO|YYm= MV:zJIRigXN? MkC1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGM{KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDBWHAuVEmWRTDhd5NigSxiRVO1NF01NjZ2IN88US=> NEjNRY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MES0N|YzPyd-MkC0OFM3Ojd:L3G+
MEF  M4fRUGZ2dmO2aX;uJIF{e2G7 NU\yWZA6OzBizszN MVyyOEBp NIP2U5NKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJG1GTiCneIDy[ZN{cW6pIIfpcIQhfHmyZTDCZ4wuOiCycn;0[YlvKGG2IEOwJJVOKGGodHXyJFI1KGi{czDifUBHUVSFLXPvcop2\2G2ZXSgZY5v\XirbjDWJIFv\CCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJGZCS1NiYX7hcJl{cXN? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODR2M{[yO{c,OjB2NEO2Nlc9N2F-
BP3 MXnBdI9xfG:|aYOgZZN{[Xl? MofCNUB1dyB{IHThfZM> M2XoNWlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iQmCzJINmdGy|IHHmeIVzKDFidH:gNkBl[Xm|IHL5JGZKXENvY3;ubpVo[XSnZDDhco5mgGmwIG[gZY5lKHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG|ZXSgSmFEWyCjbnHsfZNqeyxiRVO1NF0xNjB2Od88US=> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODR2M{[yO{c,OjB2NEO2Nlc9N2F-
M2182 NGrCU|JCdnSrdIXtc5Ih[XO|YYm= NHHNNFgyKHSxIEWgcYcwc2d? Mn23RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgUYNtNTFib4\ldoV5eHKnc4PpcochcHWvYX6gUVIyQDJiY3XscJMhgGWwb3fyZYZ1\WRiaX6gRmFNSi:lIH3veZNmKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kB1fW2xcjDzbZpmKGG2IEGgeI8hPSCvZz;r[{whcXBiYXTtbY5qe3SncnXkJFkhfGmvZYOg[ZZmenliMjDkZZl{ NXO2SnZLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC0OFM3OjdpPkKwOFQ{PjJ5PD;hQi=>
M2182 NVXQW5l{SW62aYT1cY9zKGG|c3H5 MkS1OUBu\y:tZx?= M33XWWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JG1kdC1zIH;2[ZJmgHC{ZYPzbY5oKGi3bXHuJG0zOTh{IHPlcIx{KHinbn;ndoFnfGWmIHnuJGJCVEJxYzDtc5V{\SCjc4Pld5Nm\CCjczDjc41xdGW2ZTDpcohq[mm2aX;uJI9nKHS3bX;yJIdzd3e2aDDheEA2KG2pL3vnMEBqeCCjZH3pcol{fGW{ZXSgPUB1cW2nczDleoVzgSB{IHThfZM> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODR2M{[yO{c,OjB2NEO2Nlc9N2F-
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].

Protocol (from reference)

Kinase Assay:[1]
  • Competitive fluorescence polarization assays (FPA) :

    A Bak BH3 peptide (F-BakBH3) (GQVGRQLAIIGDDINR) is labeled at the N-terminus with fluorescein isothiocyanate (FITC) and purified by HPLC. 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:[1]
  • Cell lines: PC3, H460, H1299
  • Concentrations: ~1 μM
  • Incubation Time: 72 h
  • Method: ATP-LITE assay
Animal Research:[1]
  • Animal Models: Bcl-2 transgenic mice, human prostate cancer xenografts
  • Dosages: 1 mg/kg, 3 mg/kg, 5 mg/kg
  • Administration: intraperitoneally

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 700.78
Formula

C42H40N2O8

CAS No. 1228108-65-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Sabutoclax | Sabutoclax supplier | purchase Sabutoclax | Sabutoclax cost | Sabutoclax manufacturer | order Sabutoclax | Sabutoclax distributor