2. PROTAC
  3. E3 Ligase Ligand-Linker Conjugates
  4. Lenalidomide-acetylene-C5-COOH

Lenalidomide-acetylene-C5-COOH  (Synonyms: Cereblon ligand-linker Conjugate)

Cat. No.: HY-129608 Purity: 98.32%
COA Handling Instructions

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Lenalidomide-acetylene-C5-COOH (compound 43; Cereblon ligand-linker Conjugate) is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-acetylene-C5-COOH can be connected to the ligand for protein by a linker to form PROTAC. Lenalidomide-acetylene-C5-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.

Lenalidomide-acetylene-C5-COOH Chemical Structure

Lenalidomide-acetylene-C5-COOH Chemical Structure

CAS No. : 2429878-72-6

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Based on 1 publication(s) in Google Scholar

Lenalidomide-acetylene-C5-COOH Related Antibodies

Top Publications Citing Use of Products

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

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

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Description

Lenalidomide-acetylene-C5-COOH (compound 43; Cereblon ligand-linker Conjugate) is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-acetylene-C5-COOH can be connected to the ligand for protein by a linker to form PROTAC[1]. Lenalidomide-acetylene-C5-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[1]

Cereblon

 

Molecular Weight

382.41

Formula

C21H22N2O5
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1N(C2C(NC(CC2)=O)=O)CC3=C1C=CC=C3C#CCCCCCC(O)=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 : 115 mg/mL (300.72 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 2.6150 mL 13.0750 mL 26.1499 mL
5 mM 0.5230 mL 2.6150 mL 5.2300 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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
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    90% (20% SBE-β-CD in Saline)

    Solubility: 5 mg/mL (13.07 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (13.07 mM); Clear solution

    This protocol yields a clear solution of ≥ 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 (50.0 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

Purity: 98.32%

COA (252 KB) HNMR (558 KB) LCMS (299 KB)

Handling Instructions (2659 KB)
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 2.6150 mL 13.0750 mL 26.1499 mL 65.3749 mL
5 mM 0.5230 mL 2.6150 mL 5.2300 mL 13.0750 mL
10 mM 0.2615 mL 1.3075 mL 2.6150 mL 6.5375 mL
15 mM 0.1743 mL 0.8717 mL 1.7433 mL 4.3583 mL
20 mM 0.1307 mL 0.6537 mL 1.3075 mL 3.2687 mL
25 mM 0.1046 mL 0.5230 mL 1.0460 mL 2.6150 mL
30 mM 0.0872 mL 0.4358 mL 0.8717 mL 2.1792 mL
40 mM 0.0654 mL 0.3269 mL 0.6537 mL 1.6344 mL
50 mM 0.0523 mL 0.2615 mL 0.5230 mL 1.3075 mL
60 mM 0.0436 mL 0.2179 mL 0.4358 mL 1.0896 mL
80 mM 0.0327 mL 0.1634 mL 0.3269 mL 0.8172 mL
100 mM 0.0261 mL 0.1307 mL 0.2615 mL 0.6537 mL
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Lenalidomide-acetylene-C5-COOH 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:

Lenalidomide-acetylene-C5-COOH2429878-72-6Cereblon ligand-linker ConjugateE3 Ligase Ligand-Linker ConjugatesInhibitorinhibitorinhibit

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