| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
CRBN (cereblon), an E3 ubiquitin ligase.
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|---|---|
| ln Vitro |
As a cereblon-binding intermediate, Thalidomide-piperazine-Boc itself has no intrinsic biological activity; its function is to serve as a synthetic precursor. When deprotected and conjugated to a BCL6 ligand via a linker, the resulting PROTAC can recruit the cereblon E3 ligase complex to BCL6, leading to ubiquitination and degradation of BCL6.
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| ln Vivo |
No specific in vivo activity has been reported for this intermediate alone; its in vivo degradation activity is observed only when incorporated into a complete BCL6 PROTAC molecule. The in vivo efficacy of such a BCL6 PROTAC is typically evaluated in animal models of BCL6-driven lymphomas.
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| Enzyme Assay |
N/A; this compound is not assessed in isolated enzyme/receptor binding assays. As a synthetic intermediate, its quality is confirmed by analytical methods such as HPLC and NMR, with a standard purity of ≥98%. Its structure is verified by mass spectrometry.
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| Cell Assay |
N/A; this intermediate is not tested alone in cell-based assays but is used as a building block for constructing BCL6 PROTACs. In a typical synthesis, the Boc group is removed under acidic conditions to reveal a piperazine amine, which is then conjugated to a linker and a BCL6 ligand. The resulting PROTAC is tested in BCL6-expressing cells for degradation activity.
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| Animal Protocol |
N/A; no animal studies are performed with the intermediate alone. In vivo efficacy studies for a BCL6 PROTAC synthesized from this intermediate would be conducted in mouse xenograft models of BCL6-driven lymphomas.
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| ADME/Pharmacokinetics |
This compound has a molecular weight of 442.47, a molecular formula of C22H26N4O6, and appears as a light yellow to yellow solid powder. It is typically stored as a powder at -20degC for up to 3 years or in a solvent at -80degC for 6 months. It is soluble in DMSO (41.67 mg/mL). The LogP is 1.1, and the product should be stored at 2-8degC.
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| Toxicity/Toxicokinetics |
This product is for research use only and is not for human or veterinary use. Standard chemical safety precautions should be followed during handling. The compound should be stored away from moisture.
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| References | |
| Additional Infomation |
BCL6 is a transcriptional repressor that is frequently dysregulated in diffuse large B-cell lymphoma (DLBCL) and other B-cell malignancies. Thalidomide-piperazine-Boc is a key building block for the development of BCL6-targeting PROTACs, which offer a novel therapeutic strategy for treating BCL6-driven cancers by degrading the protein rather than merely inhibiting its activity. The piperazine ring provides a versatile handle for linker attachment.
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| Molecular Formula |
C22H26N4O6
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|---|---|
| Molecular Weight |
442.4650
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| Exact Mass |
442.185
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| CAS # |
2222114-64-7
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| PubChem CID |
134413912
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
1.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
32
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| Complexity |
829
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)(C)OC(=O)N1CCN(CC1)C2=CC3=C(C=C2)C(=O)N(C3=O)C4CCC(=O)NC4=O
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| InChi Key |
PMKVKOLFYHLKAP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H26N4O6/c1-22(2,3)32-21(31)25-10-8-24(9-11-25)13-4-5-14-15(12-13)20(30)26(19(14)29)16-6-7-17(27)23-18(16)28/h4-5,12,16H,6-11H2,1-3H3,(H,23,27,28)
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| Chemical Name |
tert-butyl 4-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]piperazine-1-carboxylate
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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 :~41.67 mg/mL (~94.18 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.70 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2600 mL | 11.3002 mL | 22.6004 mL | |
| 5 mM | 0.4520 mL | 2.2600 mL | 4.5201 mL | |
| 10 mM | 0.2260 mL | 1.1300 mL | 2.2600 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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