BMS202

Catalog No.S7912 Batch:S791202

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Technical Data

Formula

C25H29N3O3

Molecular Weight 419.52 CAS No. 1675203-84-5
Solubility (25°C)* In vitro DMSO 83 mg/mL (197.84 mM)
Ethanol 83 mg/mL (197.84 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 40 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 5%Tween80 90%ddH2O
1.1mg/ml Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clarified DMSO stock solution to 50 μL of Tween80, mix evenly to clarify; then continue to add 900 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 BMS202 is a small-molecule PD-1/PD-L1 interaction inhibitor with IC50 of 18 nM.
Targets
PD-1/PD-L1 interaction [2]
(Cell-free assay)
0.018 μM
In vitro

BMS-202 inhibits PD-1/PD-L1 binding in SCC-3 and Jurkat cells with IC50 of 15 μM and 10 μM, respectively.

In vivo

BMS-202 treatment shows a clear antitumor effect compared with the controls, in humanized MHC- dKO NOG mice.

Protocol (from reference)

Cell Assay:

[3]

  • Cell lines

    SCC-3 and Jurkat cells

  • Concentrations

    IC50 of 15 μM and 10 μM

  • Incubation Time

    4 days

  • Method

    Cells were treated with various concentrations of drug for 4 days.

Animal Study:

[3]

  • Animal Models

    NOG-dKO mice

  • Dosages

    20 mg/kg

  • Administration

    i.p.

Selleck's BMS202 has been cited by 22 publications

Uncovering the colorectal cancer immunotherapeutic potential: Evening primrose (Oenothera biennis) root extract and its active compound oenothein B targeting the PD-1/PD-L1 blockade [ Phytomedicine, 2024, 125:155370] PubMed: 38266440
Development and In Vivo Evaluation of Small-Molecule Ligands for Positron Emission Tomography of Immune Checkpoint Modulation Targeting Programmed Cell Death 1 Ligand 1 [ J Med Chem, 2024, 67(5):4036-4062] PubMed: 38442487
Isolation and Total Synthesis of PM170453, a New Cyclic Depsipeptide Isolated from Lyngbya sp [ Mar Drugs, 2024, 22(7)303] PubMed: 39057411
Theoretical and experimental studies on the interaction of biphenyl ligands with human and murine PD-L1: Up-to-date clues for drug design [ Comput Struct Biotechnol J, 2023, 21:3355-3368] PubMed: 37384351
Turning a Tumor Microenvironment Pitfall into Opportunity: Discovery of Benzamidoxime as PD-L1 Ligand with pH-Dependent Potency [ Int J Mol Sci, 2023, 24(6)5535] PubMed: 36982608
Turning a Tumor Microenvironment Pitfall into Opportunity: Discovery of Benzamidoxime as PD-L1 Ligand with pH-Dependent Potency [ Int J Mol Sci, 2023, 24(6)5535] PubMed: 36982608
Development of a 68Gallium-Labeled D-Peptide PET Tracer for Imaging Programmed Death-Ligand 1 Expression [ J Vis Exp, 2023, (192).] PubMed: 36806629
Whole-body PET tracking of a d-dodecapeptide and its radiotheranostic potential for PD-L1 overexpressing tumors [ Acta Pharm Sin B, 2022, 12(3):1363-1376] PubMed: 35530129
Therapeutic targeting of PD-1/PD-L1 blockade by novel small-molecule inhibitors recruits cytotoxic T cells into solid tumor microenvironment [ J Immunother Cancer, 2022, 10(7)e004695] PubMed: 35863821
Inhibition of PD-1 Alters the SHP1/2-PI3K/Akt Axis to Decrease M1 Polarization of Alveolar Macrophages in Lung Ischemia-Reperfusion Injury [ Inflammation, 2022, 10.1007/s10753-022-01762-6] PubMed: 36357527

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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.