Thalidomide-propargyl

Name: Thalidomide-propargyl
Brand: MedChemExpress
SKU: HY-126457
Rating: 4.5 (1 reviews)

Cat. No.: HY-126457 Purity: 99.97%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Thalidomide-propargyl is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-propargyl can be connected to the ligand for protein by a linker to form the IMiD containing PROTACs. Thalidomide-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.

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

Thalidomide-propargyl Chemical Structure

CAS No. : 2098487-39-7

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
2 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 135	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 430	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 690	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Thalidomide-propargyl is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-propargyl can be connected to the ligand for protein by a linker to form the IMiD containing PROTACs^[1]. Thalidomide-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

312.28

Formula

C₁₆H₁₂N₂O₅

CAS No.

2098487-39-7

Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3OCC#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	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 16.67 mg/mL (53.38 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	3.2023 mL	16.0113 mL	32.0225 mL
5 mM	0.6405 mL	3.2023 mL	6.4045 mL
10 mM	0.3202 mL	1.6011 mL	3.2023 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)

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: ≥ 1.67 mg/mL (5.35 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: ≥ 1.67 mg/mL (5.35 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: ≥ 1.67 mg/mL (5.35 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 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 (16.7 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: 99.97%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (253 KB) HNMR (258 KB) LCMS (113 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	3.2023 mL	16.0113 mL	32.0225 mL	80.0564 mL
	5 mM	0.6405 mL	3.2023 mL	6.4045 mL	16.0113 mL
	10 mM	0.3202 mL	1.6011 mL	3.2023 mL	8.0056 mL
	15 mM	0.2135 mL	1.0674 mL	2.1348 mL	5.3371 mL
	20 mM	0.1601 mL	0.8006 mL	1.6011 mL	4.0028 mL
	25 mM	0.1281 mL	0.6405 mL	1.2809 mL	3.2023 mL
	30 mM	0.1067 mL	0.5337 mL	1.0674 mL	2.6685 mL
	40 mM	0.0801 mL	0.4003 mL	0.8006 mL	2.0014 mL
	50 mM	0.0640 mL	0.3202 mL	0.6405 mL	1.6011 mL