Home Apoptosis Bcl-2 inhibitor S55746 For research use only.

S55746

Synonyms: S 055746,BCL201

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

S55746 Chemical Structure

CAS No. 1448584-12-0

Purity & Quality Control

Batch: S875901 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.73%
99.73

S55746 Related Products

Signaling Pathway

Bcl-2 Signaling Pathways

Bcl-2 Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models RS4;11 tumor xenografts (Female SCID mice inoculated with RS4;11 cells)
Dosages 25 and 100 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02603445 Completed
Follicular Lymphoma Mantle Cell Lymphoma
Novartis Pharmaceuticals|Novartis
 November 16 2015 Phase 1
NCT02920541 Completed
Acute Myeloid Leukaemia (AML)|Myelodysplastic Syndrome (MDS)
Institut de Recherches Internationales Servier|ADIR a Servier Group company|Servier
 January 2015 Phase 1
NCT02920697 Completed
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

Chemical Information & Solubility

Molecular Weight 710.82 Formula

C43H42N4O6
CAS No. 1448584-12-0 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (140.68 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : 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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