BMS202 PD-1/PD-L1 inhibitor

Cat.No.S7912

BMS202 is a small-molecule PD-1/PD-L1 interaction inhibitor with IC50 of 18 nM.
BMS202 PD-1/PD-L1 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 419.52

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BL21(DE3) Function assay Binding affinity to [15N-Tyr]-labeled human PD-L1 (18 to 134 residues) expressed in Escherichia coli BL21(DE3) by 1H-15N 2D HMQC NMR spectroscopic analysis. 28613862
BL21(DE3) Function assay Binding affinity to [15N-Val]-labeled human PD-L1 (18 to 134 residues) expressed in Escherichia coli BL21(DE3) by 1H-15N 2D HMQC NMR spectroscopic analysis. 28613862
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 419.52 Formula

C25H29N3O3

Storage (From the date of receipt)
CAS No. 1675203-84-5 Download SDF Storage of Stock Solutions

Synonyms PD-1/PD-L1 inhibitor 2 Smiles CC1=C(C=CC=C1C2=CC=CC=C2)COC3=NC(=C(C=C3)CNCCNC(=O)C)OC

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (197.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 83 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
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.

References

Tech Support

Handling Instructions

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Frequently Asked Questions

Question 1:
I would like to know the difference of S8158, S7912, S7911, and the reason of why the IC50 is different for it.

Answer:
It is a small-molecule inhibitor and one of three different PD-L1/PD-L1 inhibitors. These three compounds have different structures, characteristics, and probably function through different mechanisms. And this is why the IC50s are different. Inhibitor 1 and 2 are also small-molecule inhibitors while inhibitor 3 is a macrocyclic inhibitor.