1. PROTAC
  2. Ligands for Target Protein for PROTAC
  3. BMS-1166-N-piperidine-COOH

BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor 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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BMS-1166-N-piperidine-COOH Chemical Structure

BMS-1166-N-piperidine-COOH Chemical Structure

CAS No. : 2447066-00-2

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Based on 1 publication(s) in Google Scholar

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Description

BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1[1]. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation[2].

Molecular Weight

639.14

Formula

C37H35ClN2O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1N(CCCC1)CC2=CC(Cl)=C(C=C2OCC3=CC=CC(C#N)=C3)OCC4=CC=CC(C5=CC=C6OCCOC6=C5)=C4C)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (156.46 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 1.5646 mL 7.8230 mL 15.6460 mL
5 mM 0.3129 mL 1.5646 mL 3.1292 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
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 (sealed storage, away from moisture and 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 1.5646 mL 7.8230 mL 15.6460 mL 39.1151 mL
5 mM 0.3129 mL 1.5646 mL 3.1292 mL 7.8230 mL
10 mM 0.1565 mL 0.7823 mL 1.5646 mL 3.9115 mL
15 mM 0.1043 mL 0.5215 mL 1.0431 mL 2.6077 mL
20 mM 0.0782 mL 0.3912 mL 0.7823 mL 1.9558 mL
25 mM 0.0626 mL 0.3129 mL 0.6258 mL 1.5646 mL
30 mM 0.0522 mL 0.2608 mL 0.5215 mL 1.3038 mL
40 mM 0.0391 mL 0.1956 mL 0.3912 mL 0.9779 mL
50 mM 0.0313 mL 0.1565 mL 0.3129 mL 0.7823 mL
60 mM 0.0261 mL 0.1304 mL 0.2608 mL 0.6519 mL
80 mM 0.0196 mL 0.0978 mL 0.1956 mL 0.4889 mL
100 mM 0.0156 mL 0.0782 mL 0.1565 mL 0.3912 mL
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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.

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Product Name:
BMS-1166-N-piperidine-COOH
Cat. No.:
HY-131187
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