1. Immunology/Inflammation Apoptosis
  2. PD-1/PD-L1 Apoptosis
  3. BMS-202

BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity.

For research use only. We do not sell to patients.

BMS-202 Chemical Structure

BMS-202 Chemical Structure

CAS No. : 1675203-84-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 145 In-stock
Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Solid
5 mg USD 132 In-stock
10 mg USD 211 In-stock
25 mg USD 436 In-stock
50 mg USD 766 In-stock
100 mg USD 1254 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of BMS-202:

Top Publications Citing Use of Products

    BMS-202 purchased from MedChemExpress. Usage Cited in: Drug Dev Res. 2021 Jul 26.  [Abstract]

    Cultured Lβt2 cells are treated with 25 μM BMS-202 and collected at 24 h. the p-p38 MAPK, p38 MAPK, p-JNK, JNK, p-ERK, ERK, and α-tubulin protein levels are detected by Western Blotting.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity[1][2].

    IC50 & Target

    IC50: 18 nM (PD-1/PD-L1)[1]
    KD: 8 μM (PD-1/PD-L1)[1]

    In Vitro

    BMS-202 (0-100 μM; 4 days; SCC-3 or Jurkat cells) treatment inhibits the proliferation of strongly PD-L1-positive SCC-3 cells (IC50 of 15 μM) and anti-CD3 antibody-activated Jurkat cells (IC50 10 μM) in vitro[2].
    BMS-202 selectively induces thermal stabilization of PD-L1. BMS-202 induces dimerization of PD-L1 in solution.BMS-202 is located at the center of the homodimer filling a deep hydrophobic pocket contributing multiple additional interactions between the monomers. BMS-202 interacts with both PD-L1 molecules using hydrophobic surfaces physiologically involved in the PD-1/PD-L1 interaction[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Proliferation Assay[2]

    Cell Line: SCC-3 or Jurkat cells
    Concentration: 0-100 μM
    Incubation Time: 4 days
    Result: Inhibited the proliferation of strongly PD-L1-positive SCC-3 cells (IC50 of 15 μM) and anti-CD3 antibody-activated Jurkat cells (IC50 10 μM) in vitro.
    In Vivo

    BMS-202 (20 mg/kg; intraperitoneal injection; daily; for 9 days; NOG-dKO mice) treatment shows a clear antitumor effect compared with the controls, in humanized MHC- dKO NOG mice[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: NOG-dKO mice (8-week-old) injected with SCC-3 cells[2]
    Dosage: 20 mg/kg
    Administration: Intraperitoneal injection; daily; for 9 days
    Result: Showed 41% growth inhibitory activity against humanized mouse-transplanted human lymphoma SCC-3 cells.
    Molecular Weight

    419.52

    Formula

    C25H29N3O3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(NCCNCC1=CC=C(OCC2=C(C)C(C3=CC=CC=C3)=CC=C2)N=C1OC)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (238.37 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3837 mL 11.9184 mL 23.8368 mL
    5 mM 0.4767 mL 2.3837 mL 4.7674 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    Volume (final)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.96 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.96 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  45% PEG300    5% Tween-80    50% Saline

      Solubility: 4.05 mg/mL (9.65 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.39%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3837 mL 11.9184 mL 23.8368 mL 59.5919 mL
    5 mM 0.4767 mL 2.3837 mL 4.7674 mL 11.9184 mL
    10 mM 0.2384 mL 1.1918 mL 2.3837 mL 5.9592 mL
    15 mM 0.1589 mL 0.7946 mL 1.5891 mL 3.9728 mL
    20 mM 0.1192 mL 0.5959 mL 1.1918 mL 2.9796 mL
    25 mM 0.0953 mL 0.4767 mL 0.9535 mL 2.3837 mL
    30 mM 0.0795 mL 0.3973 mL 0.7946 mL 1.9864 mL
    40 mM 0.0596 mL 0.2980 mL 0.5959 mL 1.4898 mL
    50 mM 0.0477 mL 0.2384 mL 0.4767 mL 1.1918 mL
    60 mM 0.0397 mL 0.1986 mL 0.3973 mL 0.9932 mL
    80 mM 0.0298 mL 0.1490 mL 0.2980 mL 0.7449 mL
    100 mM 0.0238 mL 0.1192 mL 0.2384 mL 0.5959 mL
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    BMS-202 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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