research use only
Cat.No.S7912
| Related Targets | CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor |
|---|---|
| Other PD-1/PD-L1 Inhibitors | AUNP-12 BMS-1 PD-1/PD-L1 Inhibitor 3 BMS-1166 SR 0987 INCB086550 GS-4224 CA-170 (AUPM-170) BMS-1001 Sanguisorbae Radix Extract |
| 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 | ||||||
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In vitro |
DMSO
: 83 mg/mL
(197.84 mM)
Ethanol : 83 mg/mL Water : Insoluble |
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In vivo |
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Calculation results:
Working concentration: mg/ml;
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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.
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| Molecular Weight | 419.52 | Formula | C25H29N3O3 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 1675203-84-5 | Download SDF | Storage of Stock Solutions |
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| 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 | ||
| Targets/IC50/Ki |
PD-1/PD-L1 interaction
(Cell-free assay) 0.018 μM
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|---|---|
| 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 |
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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.