Iberdomide (Synonyms: CC-220) |
カタログ番号GC19195
One-Click Copy Product Info
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イベルドマイド (CC-220) は、セレブロン結合親和性に対する IC50 が ~150nM である、経口で活性で強力なセレブロン (CRBN) E3 リガーゼ モジュレーター (CELMoD) です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1323403-33-3
Sample solution is provided at 25 µL, 10mM.
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Iberdomide (CC-220) is a cereblon modulator with an IC50 of 60 nM.
Lenalidomide and pomalidomide, targeting cereblon, are immunomodulatory drugs that are clinically effective in the treatment of cancer, including newly diagnosed and relapsed multiple myeloma. Iberdomide contains a glutarimide ring that binds in the try-tryptophan pocket of cereblon and an isoindolinone ring that can interact with both cereblon and substrates. Treatment with Iberdomide results in the loss of Ikaros and Aiolos protein levels with EC50s of 1 nM and 0.5 nM [1].
Iberdomide (CC-220) is currently in phase 2 clinical trials for the treatment of systematic lupus erythematosus (SLE) and phase 1b/2a clinical trials for relapsed and refractory multiple myeloma (MM)[1].
References:
[1]. Matyskiela ME, et al. A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos. J Med Chem. 2017 Apr 20.
Kinase experiment: | Iberdomide is dissolved in DMSO. In the assay, 60 nM 6Xhis-tagged CRBN-DDB1 is combined with 30 nM cy5-conjugated cereblon modulator and 3 nM LanthaScreen Eu-anti-His Tag antibody in 20 mM HEPES pH 7, 150 mM NaCl, 0.005% Tween-20 assay buffer. FRET is observed by exciting at 340 nm and monitoring emission at 615 nm and 665 nm, and FRET efficiency is determined by the ratio of FRET to non-FRET emission. Competing cereblon modulating compound (Iberdomide) or DMSO carrier is titrated and incubated for 10 min before scanning[1]. |
References: [1]. Matyskiela ME, et al. A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos. J Med Chem. 2017 Apr 20. | |
| Cas No. | 1323403-33-3 | SDF | |
| 同義語 | CC-220 | ||
| Canonical SMILES | O=C([C@@H](N(CC1=C2C=CC=C1OCC3=CC=C(CN4CCOCC4)C=C3)C2=O)CC5)NC5=O | ||
| Formula | C25H27N3O5 | M.Wt | 449.5 |
| 溶解度 | DMSO : ≥ 30 mg/mL (66.74 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2247 mL | 11.1235 mL | 22.2469 mL |
| 5 mM | 444.9 μL | 2.2247 mL | 4.4494 mL |
| 10 mM | 222.5 μL | 1.1123 mL | 2.2247 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)