2. Immunology/Inflammation
  3. PD-1/PD-L1
  4. BMS-8

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.

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BMS-8

BMS-8 構造式

CAS 番号 : 1675201-90-7

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 103 在庫あり
Solution
10 mM * 1 mL in DMSO USD 103 在庫あり
Solid
5 mg $95 在庫あり
10 mg $165 在庫あり
25 mg $300 在庫あり
50 mg $460 在庫あり
100 mg $680 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

BMS-8 関連抗体

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  • 生物活性

  • 純度とドキュメンテーション

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製品説明

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[1].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
6 μM
Compound: BMS-8
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
[PMID: 30878834]
HEK293 IC50
146 nM
Compound: BMS-8
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 PDL1 followed by PD1 addition and measured after 15 mins by APC-labeled anti-His antibody/Eu-labeled anti-human IgG based HTRF assay
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 PDL1 followed by PD1 addition and measured after 15 mins by APC-labeled anti-His antibody/Eu-labeled anti-human IgG based HTRF assay
[PMID: 32667799]
HEK293 IC50
60 μM
Compound: BMS-8
Antiproliferative activity against HEK293 cells incubated for 2 days by MTT assay
Antiproliferative activity against HEK293 cells incubated for 2 days by MTT assay
[PMID: 30878834]
HT-29 IC50
19 μM
Compound: BMS-8
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
[PMID: 30878834]
HeLa IC50
> 100 μM
Compound: BMS-8
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
[PMID: 30878834]
MCF7 IC50
20 μM
Compound: BMS-8
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
[PMID: 30878834]
体外実験

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.

BMS-8 関連抗体
分子量

494.42

分子式

C27H28BrNO3
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(C=CC=C1C2=CC=CC=C2)COC3=CC=C(C=C3Br)CN4CCCCC4C(O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0226 mL 10.1129 mL 20.2257 mL
5 mM 0.4045 mL 2.0226 mL 4.0451 mL
10 mM 0.2023 mL 1.0113 mL 2.0226 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
参考文献

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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BMS-8 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-81675201-90-7BMS8BMS 8PD-1/PD-L1PD-1/Programmed death-ligand 1PD-1PD-L1PPI,Inhibitorinhibitorinhibit

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製品名:
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製品番号:
HY-116274
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