2. PROTAC Autophagy Apoptosis
  3. E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis
  4. Thalidomide-NH-PEG3-NH-Boc

Thalidomide-NH-PEG3-NH-Boc is an E3 Ligase Ligand-Linker Conjugate consisting of Thalidomide (HY-14658) and NH-PEG3-NH-Boc. Thalidomide-NH-PEG3-NH-Boc acts as a ligand for Cereblon to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-NH-PEG3-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-NH-PEG3-NH-Boc is a key intermediate in the synthesis of CRBN-based PROTAC molecules.

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Thalidomide-NH-PEG3-NH-Boc Chemical Structure

Thalidomide-NH-PEG3-NH-Boc Chemical Structure

CAS No. : 2204246-03-5

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5 mg USD 55 In-stock
10 mg USD 90 In-stock
25 mg USD 185 In-stock
50 mg USD 300 In-stock
100 mg USD 480 In-stock
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Based on 1 publication(s) in Google Scholar

Thalidomide-NH-PEG3-NH-Boc Related Antibodies

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von Hippel-Lindau (VHL) MDM2 Cereblon cIAP1 Aryl Hydrocarbon Receptor

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Description

Thalidomide-NH-PEG3-NH-Boc is an E3 Ligase Ligand-Linker Conjugate consisting of Thalidomide (HY-14658) and NH-PEG3-NH-Boc. Thalidomide-NH-PEG3-NH-Boc acts as a ligand for Cereblon to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-NH-PEG3-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-NH-PEG3-NH-Boc is a key intermediate in the synthesis of CRBN-based PROTAC molecules.

IC50 & Target

Cereblon

 

Molecular Weight

548.59

Formula

C26H36N4O9
CAS No.
Appearance

Oil

Color

Light yellow to yellow

SMILES

O=C(OC(C)(C)C)NCCOCCOCCOCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -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 (182.29 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 1.8229 mL 9.1143 mL 18.2285 mL
5 mM 0.3646 mL 1.8229 mL 3.6457 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
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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 (4.56 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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).
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 1.8229 mL 9.1143 mL 18.2285 mL 45.5714 mL
5 mM 0.3646 mL 1.8229 mL 3.6457 mL 9.1143 mL
10 mM 0.1823 mL 0.9114 mL 1.8229 mL 4.5571 mL
15 mM 0.1215 mL 0.6076 mL 1.2152 mL 3.0381 mL
20 mM 0.0911 mL 0.4557 mL 0.9114 mL 2.2786 mL
25 mM 0.0729 mL 0.3646 mL 0.7291 mL 1.8229 mL
30 mM 0.0608 mL 0.3038 mL 0.6076 mL 1.5190 mL
40 mM 0.0456 mL 0.2279 mL 0.4557 mL 1.1393 mL
50 mM 0.0365 mL 0.1823 mL 0.3646 mL 0.9114 mL
60 mM 0.0304 mL 0.1519 mL 0.3038 mL 0.7595 mL
80 mM 0.0228 mL 0.1139 mL 0.2279 mL 0.5696 mL
100 mM 0.0182 mL 0.0911 mL 0.1823 mL 0.4557 mL
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Thalidomide-NH-PEG3-NH-Boc 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:

Thalidomide-NH-PEG3-NH-Boc2204246-03-5E3 Ligase Ligand-Linker ConjugatesAutophagyApoptosisInhibitorinhibitorinhibit

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