1. PROTAC
  2. E3 Ligase Ligand-Linker Conjugates
  3. Lenalidomide-C5-NH2

Lenalidomide-C5-NH2 is an E3 ligase ligand-linker conjugate. Lenalidomide-C5-NH2 can be coupled to a target protein ligand via a linker to form a PROTAC molecule—such as a PROTAC degrader for MDM2.

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Lenalidomide-C5-NH2

Lenalidomide-C5-NH2 Chemical Structure

CAS No. : 2093388-45-3

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Description

Lenalidomide-C5-NH2 is an E3 ligase ligand-linker conjugate. Lenalidomide-C5-NH2 can be coupled to a target protein ligand via a linker to form a PROTAC molecule—such as a PROTAC degrader for MDM2[1][2].

IC50 & Target[1]

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.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

329.40

Formula

C18H23N3O3

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NC(=O)C(N2C(=O)C3=CC=CC(=C3C2)CCCCCN)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (151.79 mM; Need ultrasonic)

DMSO : 5 mg/mL (15.18 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 3.0358 mL 15.1791 mL 30.3582 mL
5 mM 0.6072 mL 3.0358 mL 6.0716 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.5 mg/mL (1.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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: ≥ 0.5 mg/mL (1.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
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 (stored under nitrogen). 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 / H2O 1 mM 3.0358 mL 15.1791 mL 30.3582 mL 75.8956 mL
5 mM 0.6072 mL 3.0358 mL 6.0716 mL 15.1791 mL
10 mM 0.3036 mL 1.5179 mL 3.0358 mL 7.5896 mL
15 mM 0.2024 mL 1.0119 mL 2.0239 mL 5.0597 mL
H2O 20 mM 0.1518 mL 0.7590 mL 1.5179 mL 3.7948 mL
25 mM 0.1214 mL 0.6072 mL 1.2143 mL 3.0358 mL
30 mM 0.1012 mL 0.5060 mL 1.0119 mL 2.5299 mL
40 mM 0.0759 mL 0.3795 mL 0.7590 mL 1.8974 mL
50 mM 0.0607 mL 0.3036 mL 0.6072 mL 1.5179 mL
60 mM 0.0506 mL 0.2530 mL 0.5060 mL 1.2649 mL
80 mM 0.0379 mL 0.1897 mL 0.3795 mL 0.9487 mL
100 mM 0.0304 mL 0.1518 mL 0.3036 mL 0.7590 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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Product Name:
Lenalidomide-C5-NH2
Cat. No.:
HY-122725
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