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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Cereblon (CRBN), a substrate receptor for the CUL4-RBX1-DDB1 E3 ubiquitin ligase complex. The thalidomide-based ligand binds to the CRBN protein, facilitating the formation of a ternary complex between the E3 ligase and a target protein when the compound is conjugated to a target-binding warhead, leading to ubiquitination and subsequent degradation.
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| ln Vitro |
The compound itself acts as a ligand for CRBN and is not directly bioactive. When incorporated into a PROTAC (e.g., THAL-SNS-032), it enables the compound to recruit CRBN to the target protein, resulting in its ubiquitination and degradation. This mechanism allows for the selective removal of disease-causing proteins, representing a distinct approach from traditional enzyme inhibition.
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| ln Vivo |
In vivo, when used as part of a PROTAC, the compound facilitates the degradation of target proteins in animal models, leading to sustained pharmacological effects. The ability to degrade targets rather than just inhibit them can result in prolonged duration of action and the potential to overcome resistance mutations, as the entire protein is removed.
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| Enzyme Assay |
Cereblon binding assay: Recombinant human CRBN protein is immobilized on a sensor chip or plate. Increasing concentrations of Thalidomide-4-O-C10-NH2 hydrochloride (0-1000 nM) are injected, and binding affinity is measured by surface plasmon resonance (SPR) or fluorescence polarization. Non-specific binding is determined using a non-binding control compound. The IC50 for CRBN binding can be calculated via non-linear regression.
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| Cell Assay |
PROTAC-mediated degradation assay: Target protein-expressing cells are treated with a PROTAC containing Thalidomide-4-O-C10-NH2 hydrochloride (0.1-1000 nM) for 6-24 h. Cell lysates are analyzed by Western blotting using antibodies against the target protein and a loading control (e.g., GAPDH). The DC50 (half-maximal degradation concentration) is calculated by densitometry from triplicate experiments.
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| Animal Protocol |
Xenograft tumor model: Mice bearing target-positive tumor xenografts are treated with a PROTAC containing Thalidomide-4-O-C10-NH2 hydrochloride (10-50 mg/kg, i.p. or p.o., daily). Tumor volume is measured every 2-3 days. At study termination, tumors are excised for target protein level analysis by Western blot, and pharmacodynamic markers of degradation (e.g., ubiquitination) are assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for the standalone linker-ligand conjugate are not applicable, as it is not administered as a therapeutic agent. When incorporated into a PROTAC, the pharmacokinetics are influenced by the overall molecular weight and properties of the complete molecule. The compound is soluble in DMSO and is typically formulated for in vivo studies using vehicles such as DMSO/PEG300/Tween-80/saline mixtures.
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| Toxicity/Toxicokinetics |
Toxicology data for Thalidomide-4-O-C10-NH2 hydrochloride are not available, as it is a research component for PROTAC synthesis and not a therapeutic agent. The thalidomide scaffold has known teratogenic and immunomodulatory properties; however, the compound is intended for research use only. Standard safety precautions for handling chemical compounds should be followed.
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| Additional Infomation |
Thalidomide-4-O-C10-NH2 hydrochloride is a research-grade cereblon ligand and linker for PROTAC synthesis. It has not entered clinical trials or received regulatory approval for human use. The compound is used in the development of targeted protein degraders for various diseases, including cancer and inflammatory disorders. It is for research use only and should be stored at -20degC, sealed and away from moisture.
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| Molecular Formula |
C23H32CLN3O5
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| Related CAS # |
Thalidomide-4-O-C10-NH2;1957236-08-6
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| Appearance |
Typically exists as solid at room temperature
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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