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

BMS-202 

Cat. No.: HY-19745 Purity: 98.45%
Handling Instructions

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

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
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10 mg USD 192 In-stock
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25 mg USD 396 In-stock
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50 mg USD 696 In-stock
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100 mg USD 1140 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

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].

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.

1675203-84-5

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (238.37 mM)

*"≥" 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
10 mM 0.2384 mL 1.1918 mL 2.3837 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 98.45%

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Keywords:

BMS-202BMS202BMS 202PD-1/PD-L1ApoptosisPD-1/Programmed death-ligand 1Thermal stabilizationnonpeptidicdimerichydrophobicantitumoranti-proliferationimmune-responseInhibitorinhibitorinhibit

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