Thalidomide-Propargyne-PEG3-COOH

Name: Thalidomide-Propargyne-PEG3-COOH
Brand: MedChemExpress
SKU: HY-138776
Rating: 4.5 (1 reviews)

Cat. No.: HY-138776 Purity: 98.01%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Thalidomide-Propargyne-PEG3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology. Thalidomide-Propargyne-PEG3-COOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

Thalidomide-Propargyne-PEG3-COOH Chemical Structure

CAS No. : 2797649-54-6

Size	Price	Stock	Quantity
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 145	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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•Related Small Molecules:

•Related Proteins:

View All E3 Ligase Ligand-Linker Conjugates Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) MDM2 Cereblon cIAP1 Aryl Hydrocarbon Receptor TRIM21

Biological Activity
Purity & Documentation
References
Customer Review

Description

Thalidomide-Propargyne-PEG3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology^[1]. Thalidomide-Propargyne-PEG3-COOH 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

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

472.44

Formula

C₂₃H₂₄N₂O₉

CAS No.

2797649-54-6

Appearance

Viscous Liquid

Color

Light yellow to yellow

SMILES

OC(CCOCCOCCOCC#CC(C=C12)=CC=C2C(N(C1=O)C3CCC(NC3=O)=O)=O)=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 (211.67 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	2.1167 mL	10.5834 mL	21.1667 mL
5 mM	0.4233 mL	2.1167 mL	4.2333 mL
10 mM	0.2117 mL	1.0583 mL	2.1167 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.

Molarity Calculator
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: ≥ 2.5 mg/mL (5.29 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 (5.29 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 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)

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).

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

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: 98.01%

Select Batch:

Data Sheet (270 KB) SDS (252 KB)

COA (246 KB) HNMR (297 KB) LCMS (290 KB)

Handling Instructions (2659 KB)

References

[1]. Sato T, et al. Cereblon-Based Small-Molecule Compounds to Control Neural Stem Cell Proliferation in Regenerative Medicine. Front Cell Dev Biol. 2021;9:629326. Published 2021 Mar 11. [Content Brief]

[2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-988. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1167 mL	10.5834 mL	21.1667 mL	52.9168 mL
	5 mM	0.4233 mL	2.1167 mL	4.2333 mL	10.5834 mL
	10 mM	0.2117 mL	1.0583 mL	2.1167 mL	5.2917 mL
	15 mM	0.1411 mL	0.7056 mL	1.4111 mL	3.5278 mL
	20 mM	0.1058 mL	0.5292 mL	1.0583 mL	2.6458 mL
	25 mM	0.0847 mL	0.4233 mL	0.8467 mL	2.1167 mL
	30 mM	0.0706 mL	0.3528 mL	0.7056 mL	1.7639 mL
	40 mM	0.0529 mL	0.2646 mL	0.5292 mL	1.3229 mL
	50 mM	0.0423 mL	0.2117 mL	0.4233 mL	1.0583 mL
	60 mM	0.0353 mL	0.1764 mL	0.3528 mL	0.8819 mL
	80 mM	0.0265 mL	0.1323 mL	0.2646 mL	0.6615 mL
	100 mM	0.0212 mL	0.1058 mL	0.2117 mL	0.5292 mL