BMS-1166

Name: BMS-1166
Brand: MedChemExpress
SKU: HY-102011
Rating: 5.0 (6 reviews)

Cat. No.: HY-102011 Pureté: 99.49%: Fiche technique
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Instruction de manipulation
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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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CAS No. : 1818314-88-3

Size	Stock	Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
1 mg	En stock	Estimated Time of Arrival: December 31
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtenir un devis
500 mg	Obtenir un devis

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Based on 6 publication(s) in Google Scholar

Other Forms of BMS-1166:

BMS-1166 hydrochloride In-stock
BMS-1166 (Standard) Obtenir un devis

6 Publications Citing Use of MCE BMS-1166

Cell Proliferation/Viability Assay

Cell Imaging/Staining

Cell Migration/Invasion Assay

Flow Cytometry

: 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.

Recommandations en vedette

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Activité biologique
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Description

IC₅₀ & Target

IC50: 1.4 nM (PD-1/PD-L1 interaction)^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
B16-F10	DC₅₀	0.39 μM Compound: 8; BMS1166	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	[PMID: 38665824]
CHO	GI₅₀	> 30 μM Compound: BMS1166	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	[PMID: 33770574]
CHO	GI₅₀	> 30 μM Compound: BMS1166	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	[PMID: 33770574]
CT26	DC₅₀	0.35 μM Compound: 8; BMS1166	Antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability Antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability	[PMID: 38665824]
Jurkat	EC₅₀	1578 nM Compound: BMS-1166	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 addition and measured after 6 hrs by Bio-Glo reagent based luminescence microplate reader analysis 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 addition and measured after 6 hrs by Bio-Glo reagent based luminescence microplate reader analysis	[PMID: 38894909]
Jurkat	IC₅₀	0.1 nM Compound: 15; BMS-1166	Cytotoxicity against human Jurkat T cells assessed as reduction in cell viability Cytotoxicity against human Jurkat T cells assessed as reduction in cell viability	[PMID: 33517226]

In Vitro

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.

Masse moléculaire

641.11

Formule

C₃₆H₃₃ClN₂O₇

CAS No.

1818314-88-3

Appearance

Solid

Color

White to off-white

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

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5598 mL	7.7990 mL	15.5979 mL
5 mM	0.3120 mL	1.5598 mL	3.1196 mL
10 mM	0.1560 mL	0.7799 mL	1.5598 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité
Calculateur de dilution

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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 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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.24 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)

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).

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.

Pureté et documentation

Purity: 99.49%

Select Batch:

Fiche technique (274 KB) SDS (393 KB)

COA (249 KB) HNMR (146 KB) RP-HPLC (245 KB)

Instruction de manipulation (2659 KB)

Références

[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

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

BMS-1166 Related Classifications

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-11661818314-88-3BMS1166BMS 1166PD-1/PD-L1PD-1/Programmed death-ligand 1immunecheckpointdimerizationinteractionTcellactivationInhibitorinhibitorinhibit

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BMS-1166

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Other Forms of BMS-1166:

BMS-1166 Related Antibodies

6 Publications Citing Use of MCE BMS-1166

Recommandations en vedette

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Activité biologique

Pureté et documentation

Références

Avis client

BMS-1166 Related Antibodies

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

BMS-1166 Related Classifications

Keywords:

Vos produits récemment consultés:

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