| 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 |
| Targets |
Cereblon (CRBN), a substrate receptor of the CRL4 E3 ubiquitin ligase complex. The compound binds to CRBN with high affinity, recruiting the E3 ligase machinery to facilitate ubiquitination and proteasomal degradation of target proteins when incorporated into PROTACs.
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| ln Vitro |
PROTAC contains two distinct ligands linked by a single linker: one is the ligand for the E3 ubiquitin ligase, and the other is the ligand for the target protein. PROTAC utilizes the intracellular ubiquitin-proteasome system to selectively degrade the target protein.
The ligand alone has no degradation activity. It serves as a CRBN-binding warhead. In PROTAC conjugates incorporating this ligand, in vitro degradation DC50 values typically range from sub-nanomolar to low micromolar depending on the target protein, cell line, linker length, and target-binding ligand used. |
| ln Vivo |
No direct in vivo activity is reported for the ligand alone. In PROTAC conjugates incorporating this ligand, in vivo efficacy such as sustained target protein knockdown and tumor growth inhibition has been demonstrated in mouse xenograft models, typically achieved at doses of 10-100 mg/kg via IP or IV administration.
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| Enzyme Assay |
General CRBN binding assay: perform surface plasmon resonance (SPR) or biolayer interferometry (BLI) using immobilized CRBN-DDB1 protein complex. Inject serial dilutions of compound (1 nM to 10 uM) and determine binding affinity (KD, kon, koff). Alternatively, use a competitive TR-FRET assay with a fluorescent CRBN probe to determine IC50 values.
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| Cell Assay |
General cellular assay for PROTACs containing this ligand: treat target cells (e.g., HEK293T, HeLa) with 0.0001-10 uM PROTAC for 4-24 hours. Lyse cells, quantify target protein via Western blot or immunoassay. Determine DC50 (half-maximal degradation concentration) using dose-response curve fitting. Include lenalidomide or pomalidomide as competitors to confirm CRBN-dependent degradation.
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| Animal Protocol |
General animal protocol for PROTACs incorporating this ligand: administer PROTAC conjugate (10-100 mg/kg) to mice via IP or IV injection. For PK/PD studies, collect plasma, liver, and tumor tissues at 0.5, 1, 2, 4, 8, 24 hours post-dose. For efficacy studies in xenograft models, treat mice daily or every other day for 2-4 weeks, measure tumor volume twice weekly, and quantify target protein in tumors by IHC or Western blot at study endpoint.
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| ADME/Pharmacokinetics |
Lipophilic (cLogP ~2.5-3.5). Low aqueous solubility; DMSO stock solutions required. The two fluorine atoms enhance metabolic stability and may modulate binding affinity to CRBN. High plasma protein binding (>90%) predicted. Moderate clearance, short half-life (~0.5-2 hours). May have some CNS penetration depending on lipophilicity.
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| Toxicity/Toxicokinetics |
Low acute toxicity expected at typical PROTAC doses (10-100 mg/kg). However, CRBN ligands share structural similarity with lenalidomide and thalidomide, which are known teratogens and can cause immunomodulatory effects and myelosuppression. Handle with extreme caution in a certified biosafety cabinet. Not for human use.
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| Additional Infomation |
Store as a solid at -20degC under inert atmosphere for long-term storage (2 years). For short-term storage (2 weeks), keep at 4degC. Protect from light and moisture. Molecular weight: not specified; formula: not specified; CAS: 2438241-40-6. Purity typically ≥98% by HPLC. For research use only. Soluble in DMSO.
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| Molecular Formula |
C13H10F2N2O3
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|---|---|
| Molecular Weight |
280.23
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| CAS # |
2438241-40-6
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| Appearance |
Solid powder
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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) |
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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5685 mL | 17.8425 mL | 35.6850 mL | |
| 5 mM | 0.7137 mL | 3.5685 mL | 7.1370 mL | |
| 10 mM | 0.3568 mL | 1.7842 mL | 3.5685 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.
Products are for research use only; We do not sell to patients
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