S55746

Catalog No.S8759 Synonyms: S 055746,BCL201

For research use only.

S55746 (S 055746,BCL201) is a novel, orally active BCL-2 specific inhibitor (Ki = 1.3 nM) with poor affinity for BCL-XL and no significant binding to MCL-1, BFL-1 (BCL2A1/A1). The selectivity of S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds.

S55746 Chemical Structure

CAS No. 1448584-12-0

Selleck's S55746 has been cited by 1 Publication

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Biological Activity

Description S55746 (S 055746,BCL201) is a novel, orally active BCL-2 specific inhibitor (Ki = 1.3 nM) with poor affinity for BCL-XL and no significant binding to MCL-1, BFL-1 (BCL2A1/A1). The selectivity of S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds.
Targets
Bcl-2 [1]
(Cell-free assay)
1.3 nM(Ki)
In vitro

S55746 occupies the hydrophobic groove of BCL-2. In a panel of hematological cell lines, S55746 induces hallmarks of apoptosis including externalization of phosphatidylserine, caspase-3 activation and PARP cleavage. S55746 potently induces RS4;11 cell killing after 72 h of treatment with an IC50 of 71.6 nM and exhibits a much weaker activity in H146 (IC50 = 1.7 μM), a BCL-XL-dependent cell line, which expresses a low level of BCL-2 and high level of BCL-XL. It has no cytotoxic activity on BCL-XL-dependent cells, such as platelets[1].

In vivo

S55746 administered by oral route daily in mice demonstrates robust anti-tumor efficacy in two hematological xenograft models (RS4;11 and Toledo models) with no weight lost and no change in behavior[1].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: RS4;11 cells
  • Concentrations: 0.01, 0.03, 0.1, 0.3, 1 μM
  • Incubation Time: 2 hours
  • Method:

    Apoptosis induction in RS4;11 cells treated with S55746 at various concentrations for 2 h. Cells were analyzed by flow cytometry for PI and annexin V-FITC labeling.

Animal Research:

[1]

  • Animal Models: RS4;11 tumor xenografts (Female SCID mice inoculated with RS4;11 cells)
  • Dosages: 25 and 100 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 710.82
Formula

C43H42N4O6

CAS No. 1448584-12-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCN2C(=C(C=C2C3=CC4=C(C=C3C(=O)N5CC6=CC=CC=C6CC5CN7CCOCC7)OCO4)C(=O)N(C8=CC=CC=C8)C9=CC=C(C=C9)O)C1

In vivo Formulation Calculator (Clear solution)

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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.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02603445 Completed Drug: BCL201|Drug: Idelalisib Follicular Lymphoma Mantle Cell Lymphoma Novartis Pharmaceuticals|Novartis November 16 2015 Phase 1
NCT02920541 Completed Drug: S 055746 Acute Myeloid Leukaemia (AML)|Myelodysplastic Syndrome (MDS) Institut de Recherches Internationales Servier|ADIR a Servier Group company|Servier January 2015 Phase 1
NCT02920697 Completed Drug: S 55746 Chronic Lymphocytic Leukaemia (CLL)|B-Cell Non-Hodgkin Lymphoma (NHL)|Multiple Myeloma (MM) Institut de Recherches Internationales Servier|ADIR a Servier Group company|Servier March 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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