Size | Price | Stock | Qty |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Lenalidomide-OH, a hydroxylated analog of Lenalidomide which is a cereblon (CRBN) ligand used for E3 ubiquitin ligase, can be used as a E3 ligase ligand in PROTACs for the recruitment of CRBN protein. Specifically, Lenalidomide-OH can be connected via a linker to the warhead in PROTACs that target a protein for degradation. Lenalidomide (also known as Revlimid, CC-5013) is a derivative of thalidomide approved in the United States in 2005 for the treatment for myeloma and blood disorders called myelodysplastic syndromes.
ln Vitro |
PROTACs can be created by joining lentidomide-OH and the protein ligand via a linker. Cancer-promoting proteins are degraded by ubiquitination, which is induced by PROTACs[1].
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References |
[1]. Jaime-Figueroa S, et al. Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties. 2020 Feb 1;30(3):126877.
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Molecular Formula |
C₁₃H₁₂N₂O₄
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Molecular Weight |
260.25
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CAS # |
1416990-08-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C1C2C=CC(=CC=2CN1C1C(NC(CC1)=O)=O)O
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Synonyms |
LenalidomideOH Lenalidomide OH
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~13.89 mg/mL (~53.37 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.8425 mL | 19.2123 mL | 38.4246 mL | |
5 mM | 0.7685 mL | 3.8425 mL | 7.6849 mL | |
10 mM | 0.3842 mL | 1.9212 mL | 3.8425 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.