| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Cereblon (CRBN) E3 ubiquitin ligase. The thalidomide moiety binds to CRBN, while the BODIPY FL fluorophore allows for fluorescent detection. This enables the visualization of CRBN expression levels and subcellular localization in live or fixed cells.
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|---|---|
| ln Vitro |
The compound has no direct pharmacological activity beyond binding to CRBN. It is a chemical probe. Binding to CRBN does not induce degradation or other functional changes; it merely labels CRBN for imaging. In vitro, it is used at 0.5-5 uM for staining.
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| Enzyme Assay |
A non-cell binding assay is performed to confirm CRBN engagement. Purified CRBN-DDB1 complex is incubated with BODIPY FL thalidomide (0.1-1 uM) for 30 minutes. Fluorescence polarization or a TR-FRET assay using an anti-BODIPY antibody can measure binding. The compound shows high-affinity binding (KD typically <100 nM).
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| Cell Assay |
For cell studies, cells (e.g., multiple myeloma cell lines, HEK293) are seeded on coverslips or in 96-well plates. They are incubated with BODIPY FL thalidomide (0.5-5 uM) for 1-4 hours at 37degC. After washing and fixation, cells are imaged by fluorescence microscopy (ex/em ~488/510 nm). CRBN localization is observed in the nucleus and cytoplasm.
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| Animal Protocol |
No animal studies are typically performed with this probe. In principle, it could be injected intravenously or intratumorally into mice to assess CRBN expression in tumors by in vivo fluorescence imaging. However, such studies are not well-documented and would require optimization.
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| ADME/Pharmacokinetics |
The BODIPY FL fluorophore is lipophilic and cell-permeable. The thalidomide moiety directs binding to CRBN. The conjugate is expected to be taken up by cells within minutes to hours and to be retained in CRBN-expressing compartments. Formal PK studies are not available.
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| Toxicity/Toxicokinetics |
The toxicity of BODIPY FL thalidomide is expected to be low at the concentrations used for microscopy (low micromolar). BODIPY dyes are generally well-tolerated. The thalidomide component has teratogenic potential, so caution and appropriate handling (avoid skin contact, use fume hood) are required.
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| References | |
| Additional Infomation |
BODIPY FL thalidomide is a research tool for studying the expression and localization of the E3 ligase cereblon (CRBN). It is particularly useful for assessing CRBN levels in cells before performing PROTAC or molecular glue degrader experiments. It also serves as a building block for fluorescent PROTACs. For research use only. Store at -20degC protected from light.
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| Molecular Formula |
C37H43BF2N6O7
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|---|---|
| Molecular Weight |
732.581135988235
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| Exact Mass |
732.325
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| CAS # |
2740620-18-0
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| PubChem CID |
165714709
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| Appearance |
Orange to red solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
53
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| Complexity |
1590
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| Defined Atom Stereocenter Count |
0
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| SMILES |
F[B-]1(N2C(C)=CC(C)=C2C=C2C=CC(CCC(NCCCCCCCCNC(COC3=CC=CC4=C3C(N(C4=O)C3C(NC(CC3)=O)=O)=O)=O)=O)=[N+]21)F
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| InChi Key |
CJILTFJYYOHLGA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C37H43BF2N6O7/c1-23-20-24(2)45-29(23)21-26-13-12-25(46(26)38(45,39)40)14-16-31(47)41-18-7-5-3-4-6-8-19-42-33(49)22-53-30-11-9-10-27-34(30)37(52)44(36(27)51)28-15-17-32(48)43-35(28)50/h9-13,20-21,28H,3-8,14-19,22H2,1-2H3,(H,41,47)(H,42,49)(H,43,48,50)
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| Chemical Name |
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[8-[[2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyacetyl]amino]octyl]propanamide
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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 :~100 mg/mL (~136.50 mM)
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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 | 1.3650 mL | 6.8252 mL | 13.6504 mL | |
| 5 mM | 0.2730 mL | 1.3650 mL | 2.7301 mL | |
| 10 mM | 0.1365 mL | 0.6825 mL | 1.3650 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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