BMS-1166
Based on 6 publication(s) in Google Scholar
BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
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- 純度: 99.49%
- CAS 番号: 1818314-88-3
- 分子式: C36H33ClN2O7
- 分子量:641.11
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 BMS-1166
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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WB
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Cell Migration/Invasion Assay
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Flow Cytometry
生物活性
IC50: 1.4 nM (PD-1/PD-L1 interaction)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B16-F10 | DC50 |
0.39 μM
Compound: 8; BMS1166
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Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell growth
Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell growth
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[PMID: 38665824] |
| CHO | GI50 |
>30 μM
Compound: BMS1166
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Growth inhibition of CHO cells expressing PDL-1/TCRa incubated for 24 hrs by Cell Titer-Glo luminescent cell viability assay
Growth inhibition of CHO cells expressing PDL-1/TCRa incubated for 24 hrs by Cell Titer-Glo luminescent cell viability assay
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[PMID: 33770574] |
| CHO | GI50 |
>30 μM
Compound: BMS1166
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Growth inhibition of CHO cells expressing PDL-1/TCRa measured after 24 hrs co-culturing with human Jurkat cells expressing PD-1/NFAT-Luc in presence of compound by Cell Titer-Glo luminescent cell viability assay
Growth inhibition of CHO cells expressing PDL-1/TCRa measured after 24 hrs co-culturing with human Jurkat cells expressing PD-1/NFAT-Luc in presence of compound by Cell Titer-Glo luminescent cell viability assay
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[PMID: 33770574] |
| CT26 | DC50 |
0.35 μM
Compound: 8; BMS1166
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Antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability
Antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability
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[PMID: 38665824] |
| Jurkat | EC50 |
1578 nM
Compound: BMS-1166
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Inhibition of interaction of human PD-1 expressed in Jurkat T cells co-transfected with NFAT response element/human PD-L1 expressed in CHO-K1 cells co-expressing cell surface protein and TCR ligand preincubated with CHO-K1 cells followed by Jurkat cell ad
Inhibition of interaction of human PD-1 expressed in Jurkat T cells co-transfected with NFAT response element/human PD-L1 expressed in CHO-K1 cells co-expressing cell surface protein and TCR ligand preincubated with CHO-K1 cells followed by Jurkat cell ad
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[PMID: 38894909] |
| Jurkat | IC50 |
0.1 nM
Compound: 15; BMS-1166
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Cytotoxicity against human Jurkat T cells assessed as reduction in cell viability
Cytotoxicity against human Jurkat T cells assessed as reduction in cell viability
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[PMID: 33517226] |
BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM in a homogenous time-resolved fluorescence binding assay[1]. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation. BMS-1166 dose dependently abolishes the inhibition of ECs stimulation by sPD-L1[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1818314-88-3
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性状 Solid
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分子量 641.11
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分子式 C36H33ClN2O7
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Color White to off-white
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SMILES
O=C(O)[C@@H]1N(CC2=CC(Cl)=C(OCC3=CC=CC(C4=CC=C(OCCO5)C5=C4)=C3C)C=C2OCC6=CC=CC(C#N)=C6)C[C@H](O)C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Chem Biol Interact
Paris saponin VII restrains PD-L1 mediated immune evasion through the AKT1 and STAT3 signaling pathways. [Abstract]2025 May 17:111562. PMID: 40389195 -
Cells
Suppressing PD-L1 Expression via AURKA Kinase Inhibition Enhances Natural Killer Cell-Mediated Cytotoxicity against Glioblastoma. [Abstract]2024 Jul 6;13(13):1155. PMID: 38995006 -
Int J Med Sci
Dual PI3K/mTOR Inhibitor BEZ235 combined with BMS-1166 Promoting Apoptosis in Colorectal Cancer. [Abstract]2024 Jul 9;21(10):1814-1823. PMID: 39113885
BMS-1166 purchased from MedChemExpress. Usage Cited in: Int J Med Sci. 2024 Jul 9;21(10):1814-1823. [Abstract]
Cell viability of SW480 and SW480R cells treated with BMS-1166 (0.2, 0.5, 1, 2 μM) after 24 h was assessed by MTT assays.
BMS-1166 purchased from MedChemExpress. Usage Cited in: Int J Med Sci. 2024 Jul 9;21(10):1814-1823. [Abstract]
Colony formation assays were used to determine the clonogenic capacity of SW480 and SW480R cells treated with BMS-1166 (0.5 μM).
BMS-1166 purchased from MedChemExpress. Usage Cited in: Int J Med Sci. 2024 Jul 9;21(10):1814-1823. [Abstract]
Expression and phosphorylation of S6K and elF4EBP1 after treatment with BEZ235 plus BMS-1166 (0.5 μM) in SW480 and SW480R cells.
BMS-1166 purchased from MedChemExpress. Usage Cited in: Int J Med Sci. 2024 Jul 9;21(10):1814-1823. [Abstract]
Wound healing assays were carried out to assess the migration ability of CRC cells treated with BMS-1166, BEZ235, or the combination of the two drugs for 12, 24, and 48 h.
BMS-1166 purchased from MedChemExpress. Usage Cited in: Int J Med Sci. 2024 Jul 9;21(10):1814-1823. [Abstract]
CRC cells were treated with BMS-1166 for 24 h, stained with JC-1, and detected by flow cytometry.
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Biochem Biophys Res Commun
Baicalin inhibits bladder cancer progression by suppressing PD-L1-mediated M2 macrophage polarization via ALDH2. [Abstract]2025 Nov 21:794:153036. PMID: 41330073 -
Bio Protoc
Establishment of Human PD-1/PD-L1 Blockade Assay Based on Surface Plasmon Resonance (SPR) Biosensor. [Abstract]2023 Aug 5;13(15):e4765. PMID: 37575393 -
J Vis Exp
2025 May 2:(219). PMID: 40388341
溶剤 & 溶解度
DMSO : 125 mg/mL (194.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (393 KB)
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- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Guzik K, et al. Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1. J Med Chem. 2017 Jul 13;60(13):5857-5867. [Content Brief]
[2]. Skalniak L, et al. Small-molecule inhibitors of PD-1/PD-L1 immune checkpoint alleviate the PD-L1-induced exhaustion of T-cells. Oncotarget. 2017 Aug 7;8(42):72167-72181. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5598 mL | 7.7990 mL | 15.5979 mL | 38.9949 mL |
| 5 mM | 0.3120 mL | 1.5598 mL | 3.1196 mL | 7.7990 mL | |
| 10 mM | 0.1560 mL | 0.7799 mL | 1.5598 mL | 3.8995 mL | |
| 15 mM | 0.1040 mL | 0.5199 mL | 1.0399 mL | 2.5997 mL | |
| 20 mM | 0.0780 mL | 0.3899 mL | 0.7799 mL | 1.9497 mL | |
| 25 mM | 0.0624 mL | 0.3120 mL | 0.6239 mL | 1.5598 mL | |
| 30 mM | 0.0520 mL | 0.2600 mL | 0.5199 mL | 1.2998 mL | |
| 40 mM | 0.0390 mL | 0.1950 mL | 0.3899 mL | 0.9749 mL | |
| 50 mM | 0.0312 mL | 0.1560 mL | 0.3120 mL | 0.7799 mL | |
| 60 mM | 0.0260 mL | 0.1300 mL | 0.2600 mL | 0.6499 mL | |
| 80 mM | 0.0195 mL | 0.0975 mL | 0.1950 mL | 0.4874 mL | |
| 100 mM | 0.0156 mL | 0.0780 mL | 0.1560 mL | 0.3899 mL |
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