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Sabutoclax

Catalog No. T6650   CAS 1228108-65-3
Synonyms: BI-97C1

Sabutoclax (BI-97C1)(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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Sabutoclax Chemical Structure
Sabutoclax, CAS 1228108-65-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 64.00
5 mg In stock $ 155.00
10 mg In stock $ 247.00
25 mg In stock $ 497.00
50 mg In stock $ 788.00
100 mg In stock $ 1,070.00
1 mL * 10 mM (in DMSO) In stock $ 169.00
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Purity: 98.5%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Sabutoclax (BI-97C1)(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&IC50 Bcl-xL:0.31 μM, Bfl-1:0.62 μM, BCL2:0.32 μM, Mcl-1:0.2 μM
In vitro Sabutoclax (0.001-10 μM; 72 hours) inhibits the growth of human prostate cancer and lung cancer cell lines[2].
Sabutoclax (0.01-1 μM; 24-48 hours) induces apoptosis in human diffuse large B-cell lymphoma cells[2].
Sabutoclax (0-15 μM; 48 hours) upregulates the levels of pro-apoptotic proteins in chemotherapy-resistant cells[1].
In vivo Sabutoclax (1-5 mg/kg; intraperitoneal injection; every two days for a total of 18 days) reduces the growth of M2182 tumors in nude mice[2].
Kinase Assay 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 ATP-LITE assay(Only for Reference)
Synonyms BI-97C1
Molecular Weight 700.78
Formula C42H40N2O8
CAS No. 1228108-65-3

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 22 mg/mL(31.4 mM)

DMSO: 93 mg/mL (132.7 mM)

TargetMolReferences and Literature

1. Yunhui Hu, et Al. Sabutoclax, pan-active BCL-2 protein family antagonist, overcomes drug resistance and eliminates cancer stem cells in breast cancer. Cancer Lett. 2018 Jun 1:423:47-59. 2. 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 May 27; 53(10):4166-76.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Inhibitor Library

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Keywords

Sabutoclax 1228108-65-3 Apoptosis BCL BI-97C1 inhibitor inhibit

 

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