A-1331852

Catalog No.S7801 Batch:S780103

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Technical Data

Formula

C38H38N6O3S
Molecular Weight 658.81 CAS No. 1430844-80-6
Solubility (25°C)* In vitro DMSO 100 mg/mL (151.78 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.)

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Biological Activity

Description A-1331852 is a potent and selectiveBCL-XL inhibitor with Ki value less than 0.01 nM for BCL-XL and 6 nM, 4 nM, 142 nM for Bcl-2, Bcl-W, MCL-1 respectively. It may be useful in the treatment of cancer, immune and autoimmune diseases.
Targets
Bcl-xL [1]
(Cell-free assay)
<0.01 nM(Ki)
In vitro A-1331852 exhibits remarkable potency both as a single agent and in combination with TKIs in killing primary CD34+ CML cell. Also, It has remarkable potency in inducing apoptosis in these cells at low nanomolar concentrations as early as 1 h post-treatment[2].
In vivo A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model, inducing tumor regressions as a single agent[1].

Protocol (from reference)

Cell Assay:[2]
  • Cell lines

    K562 cells

  • Concentrations

    100 nM

  • Incubation Time

    0-2 h

  • Method

    Immunoprecipitation of BCL-XL is carried out in K562 cells, exposed to A-1331852 (100 nM) for 0-2 h, and the eluted complexes are immunoblotted for the indicated proteins. The input cell lysates and the immunodepleted supernatant (labeled as Flow-through) are immunoblotted to check the efficiency of the immunoprecipitation.

Animal Study:[1]
  • Animal Models

    SCID and SCID-bg mice

  • Dosages

    25 mg/kg

  • Administration

    Oral administration

Customer Product Validation

Data from [Data independently produced by , , Cancer Lett, 2018, 412:131-142]

Data from [Data independently produced by , , Mol Cancer Res, 2016, 14(12):1176-1181]

Selleck's A-1331852 has been cited by 50 publications

Gravitational and mechanical forces drive mitochondrial translation [ bioRxiv, 2024, 10.1101/2023.01.18.524628] PubMed: none
Clearance of defective muscle stem cells by senolytics restores myogenesis in myotonic dystrophy type 1 [ Nat Commun, 2023, 14(1):4033] PubMed: 37468473
Single-molecule fingerprinting of protein-drug interaction using a funneled biological nanopore [ Nat Commun, 2023, 14(1):1461] PubMed: 37015934
Increased MCL1 dependency leads to new applications of BH3-mimetics in drug-resistant neuroblastoma [ Br J Cancer, 2023, 10.1038/s41416-023-02430-8] PubMed: 37723317
ChemR23 activation reprograms macrophages toward a less inflammatory phenotype and dampens carcinoma progression [ Front Immunol, 2023, 14:1196731] PubMed: 37539056
Bcl-xL is required to protect endothelial cells latently infected with KSHV from virus induced intrinsic apoptosis [ PLoS Pathog, 2023, 19(5):e1011385] PubMed: 37163552
Targeting Bcl-xL is a potential therapeutic strategy for extranodal NK/T cell lymphoma [ iScience, 2023, 26(8):107369] PubMed: 37539026
Systematic characterization of therapeutic vulnerabilities in Multiple Myeloma with Amp1q reveals increased sensitivity to the combination of MCL1 and PI3K inhibitors [ bioRxiv, 2023, 2023.08.01.551480] PubMed: 37577538
Systematic characterization of therapeutic vulnerabilities in Multiple Myeloma with Amp1q reveals increased sensitivity to the combination of MCL1 and PI3K inhibitors [ bioRxiv, 2023, 2023.08.01.551480] PubMed: 37577538
Co-targeting of BAX and BCL-XL proteins broadly overcomes resistance to apoptosis in cancer [ Nat Commun, 2022, 13(1):1199] PubMed: 35256598

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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.