Thalidomide-O-PEG2-propargyl (Synonyms: E3 ligase Ligand-Linker Conjugates 32)

Name: Thalidomide-O-PEG2-propargyl
Brand: MedChemExpress
SKU: HY-126458
Rating: 4.5 (1 reviews)

Cat. No.: HY-126458 Purity: 98.26%: FAQs
Data Sheet SDS COA Handling Instructions

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Thalidomide-O-PEG2-propargyl (E3 ligase Ligand-Linker Conjugates 32) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology. Thalidomide-O-PEG2-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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Thalidomide-O-PEG2-propargyl Chemical Structure

CAS No. : 2098487-52-4

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Free Sample (0.1 - 0.5 mg)		Apply Now
25 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Thalidomide-O-PEG2-propargyl (E3 ligase Ligand-Linker Conjugates 32) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology^[1]. Thalidomide-O-PEG2-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target^[1]

Cereblon

Molecular Weight

400.38

Formula

C₂₀H₂₀N₂O₇

CAS No.

2098487-52-4

Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3OCCOCCOCC#C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 120 mg/mL (299.72 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	2.4976 mL	12.4881 mL	24.9763 mL
5 mM	0.4995 mL	2.4976 mL	4.9953 mL
10 mM	0.2498 mL	1.2488 mL	2.4976 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Dilution Calculator

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: ≥ 3 mg/mL (7.49 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: ≥ 3 mg/mL (7.49 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (7.49 mM); Clear solution

This protocol yields a clear solution of ≥ 3 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 (30.0 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)

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

Purity: 98.26%

Select Batch:

Data Sheet (271 KB) SDS (252 KB)

COA (248 KB) LCMS (257 KB)

Handling Instructions (2659 KB)

References

[1]. Wurz RP, et al. A "Click Chemistry Platform" for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. J Med Chem. 2018 Jan 25;61(2):453-461. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4976 mL	12.4881 mL	24.9763 mL	62.4407 mL
	5 mM	0.4995 mL	2.4976 mL	4.9953 mL	12.4881 mL
	10 mM	0.2498 mL	1.2488 mL	2.4976 mL	6.2441 mL
	15 mM	0.1665 mL	0.8325 mL	1.6651 mL	4.1627 mL
	20 mM	0.1249 mL	0.6244 mL	1.2488 mL	3.1220 mL
	25 mM	0.0999 mL	0.4995 mL	0.9991 mL	2.4976 mL
	30 mM	0.0833 mL	0.4163 mL	0.8325 mL	2.0814 mL
	40 mM	0.0624 mL	0.3122 mL	0.6244 mL	1.5610 mL
	50 mM	0.0500 mL	0.2498 mL	0.4995 mL	1.2488 mL
	60 mM	0.0416 mL	0.2081 mL	0.4163 mL	1.0407 mL
	80 mM	0.0312 mL	0.1561 mL	0.3122 mL	0.7805 mL
	100 mM	0.0250 mL	0.1249 mL	0.2498 mL	0.6244 mL

Thalidomide-O-PEG2-propargyl 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.

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Thalidomide-O-PEG2-propargyl2098487-52-4E3 ligase Ligand-Linker Conjugates 32E3 Ligase Ligand-Linker ConjugatesAutophagyApoptosisPROTACInhibitorinhibitorinhibit

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Thalidomide-O-PEG2-propargyl (Synonyms: E3 ligase Ligand-Linker Conjugates 32)

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Thalidomide-O-PEG2-propargyl Related Antibodies

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•Related Small Molecules:

•Related Proteins:

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Biological Activity

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References

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Complete Stock Solution Preparation Table

Thalidomide-O-PEG2-propargyl Related Classifications

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