1. PROTAC
  2. E3 Ligase Ligand-Linker Conjugates
  3. Thalidomide-Piperazine-PEG1-NH2

Thalidomide-Piperazine-PEG1-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Thalidomide-Piperazine-PEG1-NH2 diTFA) usually boasts enhanced water solubility and stability.

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Thalidomide-Piperazine-PEG1-NH2 Chemical Structure

Thalidomide-Piperazine-PEG1-NH2 Chemical Structure

CAS No. : 2357111-29-4

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Description

Thalidomide-Piperazine-PEG1-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].

IC50 & Target

Cereblon

 

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[2].

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

Molecular Weight

429.47

Formula

C21H27N5O5

CAS No.
SMILES

O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC(N4CCN(CCOCCN)CC4)=C3)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (582.11 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 2.3285 mL 11.6423 mL 23.2845 mL
5 mM 0.4657 mL 2.3285 mL 4.6569 mL
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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3285 mL 11.6423 mL 23.2845 mL 58.2113 mL
5 mM 0.4657 mL 2.3285 mL 4.6569 mL 11.6423 mL
10 mM 0.2328 mL 1.1642 mL 2.3285 mL 5.8211 mL
15 mM 0.1552 mL 0.7762 mL 1.5523 mL 3.8808 mL
20 mM 0.1164 mL 0.5821 mL 1.1642 mL 2.9106 mL
25 mM 0.0931 mL 0.4657 mL 0.9314 mL 2.3285 mL
30 mM 0.0776 mL 0.3881 mL 0.7762 mL 1.9404 mL
40 mM 0.0582 mL 0.2911 mL 0.5821 mL 1.4553 mL
50 mM 0.0466 mL 0.2328 mL 0.4657 mL 1.1642 mL
60 mM 0.0388 mL 0.1940 mL 0.3881 mL 0.9702 mL
80 mM 0.0291 mL 0.1455 mL 0.2911 mL 0.7276 mL
100 mM 0.0233 mL 0.1164 mL 0.2328 mL 0.5821 mL
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Thalidomide-Piperazine-PEG1-NH2 Related Classifications

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  • 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:
Thalidomide-Piperazine-PEG1-NH2
Cat. No.:
HY-138789
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