BMS-8
Based on 1 publication(s) in Google Scholar
BMS-8 inhibits the PD-1/PD-L1 interaction with IC50 of 7.2 μM. BMS-8, binds directly to PD-L1 and induces formation of PD-L1 homodimers, which in turn prevents the interaction with PD-1.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.0%
- No. CAS: 1675201-90-7
- Fòrmula: C27H28BrNO3
- Peso molecular:494.42
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) BMS-8
More
Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
6 μM
Compound: BMS-8
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Antiproliferative activity against human A549 cells incubated for 2 days by MTT assay
Antiproliferative activity against human A549 cells incubated for 2 days by MTT assay
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[PMID: 30878834] |
| HEK293 | IC50 |
146 nM
Compound: BMS-8
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Inhibition of human C-terminal Ig-Fc-tagged PD1 (Leu25 to Gln167 residues) expressed in HEK293 cells/human C-terminal epitope-His-tagged PDL1 (Phe19 to Arg238 residues) expressed in HEK293 cells protein-protein interaction preincubated for 15 mins with PD
Inhibition of human C-terminal Ig-Fc-tagged PD1 (Leu25 to Gln167 residues) expressed in HEK293 cells/human C-terminal epitope-His-tagged PDL1 (Phe19 to Arg238 residues) expressed in HEK293 cells protein-protein interaction preincubated for 15 mins with PD
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[PMID: 32667799] |
| HEK293 | IC50 |
60 μM
Compound: BMS-8
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Antiproliferative activity against HEK293 cells incubated for 2 days by MTT assay
Antiproliferative activity against HEK293 cells incubated for 2 days by MTT assay
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[PMID: 30878834] |
| HeLa | IC50 |
>100 μM
Compound: BMS-8
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Antiproliferative activity against human HeLa cells incubated for 2 days by MTT assay
Antiproliferative activity against human HeLa cells incubated for 2 days by MTT assay
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[PMID: 30878834] |
| HT-29 | IC50 |
19 μM
Compound: BMS-8
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Antiproliferative activity against human HT-29 cells incubated for 2 days by MTT assay
Antiproliferative activity against human HT-29 cells incubated for 2 days by MTT assay
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[PMID: 30878834] |
| MCF7 | IC50 |
20 μM
Compound: BMS-8
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Antiproliferative activity against human MCF7 cells incubated for 2 days by MTT assay
Antiproliferative activity against human MCF7 cells incubated for 2 days by MTT assay
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[PMID: 30878834] |
BMS-8 tends to have a more stable binding mode with one PD-L1 monomer than the other and the small-molecule inducing PD-L1 dimerization was further stabilized by the non-polar interaction of Ile54, Tyr56, Met115, Ala121, and Tyr123 on both monomers and the water bridges involved in ALys124[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1675201-90-7
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Appearance Solid
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Peso molecular 494.42
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Fòrmula C27H28BrNO3
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Color White to off-white
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SMILES
CC1=C(C=CC=C1C2=CC=CC=C2)COC3=CC=C(C=C3Br)CN4CCCCC4C(O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Acta Biomater
A CXCR4-targeted immunomodulatory nanomedicine for photodynamic amplified immune checkpoint blockade therapy against breast cancer. [Abstract]2025 Mar 26:S1742-7061(25)00223-5. PMID: 40154764
Solvente y solubilidad
DMSO : 83.33 mg/mL (168.54 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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.21 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Eun-Hye Kim, et al. Preparation of Biphenyl-Conjugated Bromotyrosine for Inhibition of PD-1/PD-L1 Immune Checkpoint Interactions. Int J Mol Sci. 2020 May 21;21(10):3639. [Content Brief]
[2]. Danfeng Shi, et al. Computational Insight Into the Small Molecule Intervening PD-L1 Dimerization and the Potential Structure-Activity Relationship. Front Chem. 2019 Nov 12;7:764. [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 (protect from light). 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 | 2.0226 mL | 10.1129 mL | 20.2257 mL | 50.5643 mL |
| 5 mM | 0.4045 mL | 2.0226 mL | 4.0451 mL | 10.1129 mL | |
| 10 mM | 0.2023 mL | 1.0113 mL | 2.0226 mL | 5.0564 mL | |
| 15 mM | 0.1348 mL | 0.6742 mL | 1.3484 mL | 3.3710 mL | |
| 20 mM | 0.1011 mL | 0.5056 mL | 1.0113 mL | 2.5282 mL | |
| 25 mM | 0.0809 mL | 0.4045 mL | 0.8090 mL | 2.0226 mL | |
| 30 mM | 0.0674 mL | 0.3371 mL | 0.6742 mL | 1.6855 mL | |
| 40 mM | 0.0506 mL | 0.2528 mL | 0.5056 mL | 1.2641 mL | |
| 50 mM | 0.0405 mL | 0.2023 mL | 0.4045 mL | 1.0113 mL | |
| 60 mM | 0.0337 mL | 0.1685 mL | 0.3371 mL | 0.8427 mL | |
| 80 mM | 0.0253 mL | 0.1264 mL | 0.2528 mL | 0.6321 mL | |
| 100 mM | 0.0202 mL | 0.1011 mL | 0.2023 mL | 0.5056 mL |
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