S55746

Catalog No.S8759 Batch:S875901

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Technical Data

Formula

C43H42N4O6
Molecular Weight 710.82 CAS No. 1448584-12-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (140.68 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

[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 Study:

[1]
  • Animal Models

    RS4;11 tumor xenografts (Female SCID mice inoculated with RS4;11 cells)

  • Dosages

    25 and 100 mg/kg

  • Administration

    p.o.

Selleck's S55746 has been cited by 3 publications

Obatoclax Rescues FUS-ALS Phenotypes in iPSC-Derived Neurons by Inducing Autophagy [ Cells, 2023, 12(18)2247] PubMed: 37759469
Obatoclax Rescues FUS-ALS Phenotypes in iPSC-Derived Neurons by Inducing Autophagy [ Cells, 2023, 10.3390/cells12182247] PubMed: 37759469
Activation of RAS/MAPK pathway confers MCL-1 mediated acquired resistance to BCL-2 inhibitor venetoclax in acute myeloid leukemia [ Signal Transduct Target Ther, 2022, 7(1):51] PubMed: 35185150

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.