2. PROTAC
  3. Target Protein Ligand-Linker Conjugates
  4. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride

BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride 

Cat. No.: HY-131386A Purity: 95.01%
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BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM.

For research use only. We do not sell to patients.

BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride Chemical Structure

BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride Chemical Structure

CAS No. : 2691796-83-3

Size Price Stock Quantity
5 mg USD 580 In-stock
10 mg USD 920 In-stock
25 mg USD 1900 In-stock
50 mg USD 3000 In-stock
100 mg USD 4800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

Other Forms of BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride:

BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM[1].

In Vitro

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride Related Antibodies
Molecular Weight

780.18

Formula

C41H45Cl3N4O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=CC=CC(COC2=CC(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)=C(C=C2CN6CCCCC6C(N7CCNCC7)=O)Cl)=C1.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (128.18 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 1.2818 mL 6.4088 mL 12.8176 mL
5 mM 0.2564 mL 1.2818 mL 2.5635 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.

  • 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)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.5 mg/mL (3.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (3.20 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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).
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.
Purity & Documentation
References

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 1.2818 mL 6.4088 mL 12.8176 mL 32.0439 mL
5 mM 0.2564 mL 1.2818 mL 2.5635 mL 6.4088 mL
10 mM 0.1282 mL 0.6409 mL 1.2818 mL 3.2044 mL
15 mM 0.0855 mL 0.4273 mL 0.8545 mL 2.1363 mL
20 mM 0.0641 mL 0.3204 mL 0.6409 mL 1.6022 mL
25 mM 0.0513 mL 0.2564 mL 0.5127 mL 1.2818 mL
30 mM 0.0427 mL 0.2136 mL 0.4273 mL 1.0681 mL
40 mM 0.0320 mL 0.1602 mL 0.3204 mL 0.8011 mL
50 mM 0.0256 mL 0.1282 mL 0.2564 mL 0.6409 mL
60 mM 0.0214 mL 0.1068 mL 0.2136 mL 0.5341 mL
80 mM 0.0160 mL 0.0801 mL 0.1602 mL 0.4005 mL
100 mM 0.0128 mL 0.0641 mL 0.1282 mL 0.3204 mL
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BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride 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-1166-N-piperidine-CO-N-piperazine2691796-83-3Target Protein Ligand-Linker ConjugatesPD-1/PD-L1immune checkpointPROTAC linkerPROTAC PD-1/PD-L1 degrader-1Inhibitorinhibitorinhibit

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BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride
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