| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Lenalidomide-OH targets cereblon (CRBN), a component of the E3 ubiquitin ligase complex. As a CRBN ligand, it recruits the E3 ligase to target proteins that are bound to the other end of a PROTAC molecule. By bringing the target protein into proximity with the E3 ligase, it induces ubiquitination and subsequent proteasomal degradation of the target protein.
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| 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].
In vitro, Lenalidomide-OH is characterized by its ability to bind to cereblon (CRBN) and function as an E3 ligase ligand in PROTAC molecules. It is a hydroxylated analog of Lenalidomide. The compound's utility as a CRBN ligand makes it a valuable building block for PROTAC research. |
| ln Vivo |
In vivo, Lenalidomide-OH is used as a building block for the synthesis of PROTAC molecules that can induce targeted protein degradation. The PROTACs incorporating this ligand can be administered to animal models to study the effects of degrading specific target proteins. Its in vivo activity is realized through the PROTAC molecules synthesized using this compound.
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| Enzyme Assay |
In vitro assays for Lenalidomide-OH typically involve binding studies with cereblon (CRBN). Recombinant CRBN protein is incubated with increasing concentrations of the compound in binding buffer. Binding affinity is measured using surface plasmon resonance (SPR), isothermal titration calorimetry (ITC), or fluorescence polarization. The compound's ability to recruit CRBN can be assessed in ternary complex formation assays.
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| Cell Assay |
For in vitro cell-based assays, Lenalidomide-OH is used in the synthesis of PROTAC molecules. Cells expressing the target protein are treated with the PROTAC. Target protein degradation is confirmed by Western blot. Cell viability is assessed by MTT or CellTiter-Glo assays. The compound's effects on downstream signaling pathways are analyzed by Western blot or qRT-PCR.
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| Animal Protocol |
In vivo animal studies with Lenalidomide-OH are conducted using PROTAC molecules synthesized from this compound. The PROTAC is administered orally or intraperitoneally to rodents. Target protein degradation in tissues is confirmed by Western blot. Pharmacodynamic effects are assessed by measuring downstream signaling and biological responses. Blood samples are collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
Lenalidomide-OH (CAS: 1416990-08-3) has a molecular weight of 260.24 g/mol and a molecular formula of C13H12N2O4. Chemical name: 3-(5-hydroxy-1-oxo-2,3-dihydro-1H-isoindol-2-yl)piperidine-2,6-dione. Appearance: solid powder. Purity: ≥95%. Storage: -20°C. The compound is a cereblon (CRBN) ligand for E3 ubiquitin ligase.
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| Toxicity/Toxicokinetics |
Lenalidomide-OH is a research compound and is not approved for human therapeutic use. As a Lenalidomide analog, it may have similar toxicity concerns, including teratogenic effects. The compound is used in very small quantities as a research reagent. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
Lenalidomide-OH is a hydroxylated analog of Lenalidomide and a cereblon (CRBN) ligand for E3 ubiquitin ligase. It is used in the recruitment of CRBN protein in PROTAC technology. It has a molecular weight of 260.24 g/mol and a molecular formula of C13H12N2O4. It is not FDA-approved and is intended for research use only.
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| Molecular Formula |
C13H12N2O4
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|---|---|
| Molecular Weight |
260.245383262634
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| Exact Mass |
260.079
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| CAS # |
1416990-08-3
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| PubChem CID |
71517902
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| Appearance |
Off-white to gray solid powder
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| LogP |
-0.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
19
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| Complexity |
436
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C2C=CC(=CC=2CN1C1C(NC(CC1)=O)=O)O
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| InChi Key |
JJUMFQGCQAUIFH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H12N2O4/c16-8-1-2-9-7(5-8)6-15(13(9)19)10-3-4-11(17)14-12(10)18/h1-2,5,10,16H,3-4,6H2,(H,14,17,18)
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| Chemical Name |
3-(6-hydroxy-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione
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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.
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