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| Targets |
BMS-986189 targets the immune checkpoint protein PD‑L1 (CD274). PD‑L1 is expressed on many cancer cells and binds to PD‑1 on T cells, delivering an inhibitory signal that suppresses T cell activation and promotes immune evasion. BMS-986189 is a macrocyclic peptide that binds selectively to PD‑L1, blocking its interaction with PD‑1. This reactivates T cell‑mediated antitumor immunity, similar to clinically approved monoclonal antibodies such as nivolumab and pembrolizumab.
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| ln Vitro |
BMS-986189 is a macrocyclic peptide that blocks the PD‑1/PD‑L1 interaction with an IC₅0 of 1.03 nM. It is a potent PD‑L1 inhibitor and a non‑competitive antagonist, meaning it binds to a different site on PD‑L1 than the natural ligand. No specific cellular activity data (e.g., T cell activation or cytokine production) are reported in the search results. The compound is a macrocyclic thioether peptide antagonist with potential for cancer research, including human lung carcinoma cells L2987.
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| ln Vivo |
No specific in vivo activity data for BMS-986189 are reported in the search results. As a macrocyclic peptide PD‑L1 inhibitor with an IC₅0 of 1.03 nM, it has potential for evaluation in animal models of cancer, such as human lung carcinoma xenografts in immunocompromised mice reconstituted with human immune cells (e.g., Hu‑PBMC‑NCG mice). The compound could be administered intravenously (IV) or subcutaneously (SC). No specific in vivo data are provided.
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| Enzyme Assay |
Binding of BMS-986189 to PD‑L1 is measured by standard in vitro biochemical assays using purified recombinant human PD‑L1 protein. A fluorescence polarization (FP) or time‑resolved fluorescence resonance energy transfer (TR‑FRET) assay is typically used. A labeled PD‑1 protein or a labeled PD‑L1‑binding peptide is used as a tracer. The compound is incubated with PD‑L1 and the tracer at graded concentrations (0.01-10,000 nM). The IC₅0 of 1.03 nM is calculated from the dose‑response curve. Selectivity against other immune checkpoint proteins (e.g., PD‑L2, CTLA‑4) can be assessed similarly.
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| Cell Assay |
For cellular assays, human lung carcinoma cells (e.g., L2987) expressing PD‑L1 are co‑cultured with human primary T cells in 96‑well plates. BMS-986189 is added at graded concentrations (0.1-1000 nM). T cell activation is assessed by measuring the production of cytokines (e.g., IL‑2, IFN‑gamma) in the culture supernatant by ELISA. T cell proliferation is measured by CFSE dilution or [3H]‑thymidine incorporation. The compound‘s ability to restore T cell function is evaluated by measuring the killing of PD‑L1‑expressing tumor cells. No specific protocols are described.
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| Animal Protocol |
No animal experiments for BMS-986189 are described in the search results. For in vivo evaluation of anti‑tumor activity, 6‑8‑week‑old female NCG (NOD‑Prkdcᵉᵐ2⁶ᶜIl2rgᵉᵐ2⁶ᶜ) mice are used. Mice are engrafted with human PBMCs (Hu‑PBMC‑NCG model) to reconstitute a human immune system, then implanted subcutaneously with human lung carcinoma cells (e.g., L2987). When tumors reach approximately 100‑150 mm3, mice are randomized and treated with BMS-986189 administered intravenously (IV) at doses of 1‑10 mg/kg twice weekly for 2‑4 weeks. Tumor volumes are measured twice weekly. Blood is collected for analysis of T cell activation markers (e.g., CD69, CD25, Ki‑67) by flow cytometry. At the study endpoint, tumors are harvested for immunohistochemistry (CD8+ T cell infiltration) and Western blot (PD‑L1 expression). No specific data are provided.
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| ADME/Pharmacokinetics |
BMS-986189 (C23H2₈N₆O4S, MW = 484.57, purity ≥98%, CAS 1629665-96-8) is a solid powder. For storage, the powder should be kept at -20 degC for up to 3 years, sealed and protected from light. For in vitro use, stock solutions in DMSO (20 mg/mL, 41.27 mM) can be stored at -80 degC for up to 6 months or at -20 degC for 1 month. For in vivo use, it can be formulated in 10% DMSO / 40% PEG300 / 5% Tween‑80 / 45% saline. No detailed PK parameters (Cmax, Tmax, half‑life, bioavailability) are reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data for BMS-986189 are reported. As a research‑grade PD‑L1 inhibitor, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling peptides should be followed. PD‑L1 inhibitors as a class (e.g., nivolumab, pembrolizumab) are approved for human use and have a well‑established safety profile; however, no formal toxicology studies (LD₅0, target organ toxicity) are available for this specific compound.
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| References | |
| Additional Infomation |
BMS-986189 is a research‑grade macrocyclic peptide inhibitor of PD‑L1. The PD‑1/PD‑L1 immune checkpoint is a key mechanism by which tumors evade immune destruction. BMS-986189 is a non‑competitive antagonist, meaning it binds to a site on PD‑L1 distinct from the PD‑1 binding site, which may offer advantages over antibodies in certain applications. BMS-986189 is one of several macrocyclic peptide inhibitors of PD‑L1 developed by Bristol‑Myers Squibb (BMS). The compound has not entered clinical trials or received regulatory approval. It is available from chemical suppliers for research use only.
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| Molecular Formula |
C91H131N21O21S
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| Molecular Weight |
1887.21
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| CAS # |
1629665-96-8
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| Appearance |
Solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (52.99 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5299 mL | 2.6494 mL | 5.2988 mL | |
| 5 mM | 0.1060 mL | 0.5299 mL | 1.0598 mL | |
| 10 mM | 0.0530 mL | 0.2649 mL | 0.5299 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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