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S55746 Bcl-2 inhibitor

Name: S55746
Brand: Selleck Chemicals
SKU: S8759
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S8759

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 this compound for BCL-2 versus BCL-XL ranges from ~70 to 400 folds.

Chemical Structure

Molecular Weight: 710.82

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.73

Related Targets	Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas
Other Bcl-2 Inhibitors	ABT-737 Navitoclax (ABT-263) S63845 Obatoclax Mesylate (GX15-070) A-1210477 TW-37 A-1331852 A-1155463 Dihydrochloride UMI-77 AZD5991

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (140.68 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (7.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of 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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.625mg/ml (0.88mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 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)

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.

Chemical Information, Storage & Stability

Molecular Weight	710.82	Formula	C₄₃H₄₂N₄O₆	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1448584-12-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	S 055746,BCL201			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

Mechanism of Action

Targets/IC₅₀/Ki	Bcl-2 (Cell-free assay) 1.3 nM(Ki)
In vitro	S55746 occupies the hydrophobic groove of BCL-2. In a panel of hematological cell lines, this compound induces hallmarks of apoptosis including externalization of phosphatidylserine, caspase-3 activation and PARP cleavage. It 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.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/29732004/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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