Iberdomide
Based on 12 publication(s) in Google Scholar
Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities.
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- 純度: 99.54%
- CAS 番号: 1323403-33-3
- 分子式: C25H27N3O5
- 分子量:449.50
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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MedChemExpress（MCE）の使用を引用している文献 Iberdomide
More- Nat Cancer. 2022 May;3(5):595-613. [Abstract]
- Cell Host Microbe. 2020 Mar.
- Nat Commun. 2022 Sep 10;13(1):5324. [Abstract]
- Blood Cancer J. 2019 Feb 11;9(2):19. [Abstract]
- Cell Rep Med. 2024 Mar 19;5(3):101472. [Abstract]
- Cell Chem Biol. 2020 Jul 16;27(7):866-876.e8. [Abstract]
- Elife. 2018 Aug 1;7:e38430. [Abstract]
- J Proteome Res. 2022 Aug 5;21(8):1842-1856. [Abstract]
- J Gastroenterol Hepatol. 2026 Mar 12. [Abstract]
- bioRxiv. 2025 Jun 19.
- University of Colorado Denver. 2024.
- University of Colorado Denver. 2024.
Customer Validation & Images
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
生物活性
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Cereblon |
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Cell Line
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Type | Value | Description | References |
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| MM1.S | IC50 |
13 nM
Compound: CC-220
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Antiproliferative activity against human MM1S cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
Antiproliferative activity against human MM1S cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
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[PMID: 31125896] |
| MV4-11 | IC50 |
>20000 nM
Compound: CC-220
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Antiproliferative activity against human MV411 cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
Antiproliferative activity against human MV411 cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
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[PMID: 31125896] |
Iberdomide (CC-220; 0.01, 0.1, 1, 10 μM; 72-96 hrs) has antiproliferative effects in a panel of multiple myeloma (MM) cell lines (EJM, H929, KMS11, KMS128M, KMS12PE, MM1.S, MM1.R, RPM-8226, U266 cells) across a range of concentrations[1].
Iberdomide (0.1 μM; 96 hrs) induces apoptosis in all MM cell lines[1].
Iberdomide (0.1 μM; 24, 48, 72 hrs) results in time-dependent increases in G0/G1 and sub-G1 cell cycle fractions on H929 cells[1].
Iberdomide leads to rapid Aiolos depletion in the KMS12BM line[1].
Iberdomide (0.1 μM) displays some anti-proliferative activity in two of the Pomalidomide-resistant (PR) lines with cereblon mutations (EJM/PR and H929/PR) along with decreased levels of cereblon protein[1].
Iberdomide (0.1-1000 nM; 72 hrs) equally induces PBMC-mediated killing of both parental MM1.S cells and MM1.S/PR cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1323403-33-3
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性状 Solid
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分子量 449.50
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分子式 C25H27N3O5
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Color White to off-white
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SMILES
O=C([C@@H](N(CC1=C2C=CC=C1OCC3=CC=C(CN4CCOCC4)C=C3)C2=O)CC5)NC5=O
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別名
CC-220
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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Nat Cancer
IKAROS and MENIN coordinate therapeutically actionable leukemogenic gene expression in MLL-r acute myeloid leukemia. [Abstract]2022 May;3(5):595-613. PMID: 35534777
Iberdomide purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 May;3(5):595-613. [Abstract]
Western blot analysis for IKAROS, CK1α and MENIN protein following treatment of MV4;11 human MLL-r AML cell line for 5 hours with increasing doses of Thalidomide, lenalidomide, Pomalidomide and iberdomide (10,100, 1000 nM), using ACTIN as a loading control.
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Nat Commun
Functional genomics uncovers the transcription factor BNC2 as required for myofibroblastic activation in fibrosis. [Abstract]2022 Sep 10;13(1):5324. PMID: 36088459
Iberdomide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Sep 10;13(1):5324. [Abstract]
Western immunoassays used to monitor changes in BNC2 levels in LX2 cells treated with 1 μM pomalidomide (Pom.), thalidomide (Thal.), CC-885, Iberdomide (Iber.) or vehicle for 24 h.
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Blood Cancer J
Identification of lenalidomide resistance pathways in myeloma and targeted resensitization using cereblon replacement, inhibition of STAT3 or targeting of IRF4. [Abstract]2019 Feb 11;9(2):19. PMID: 30741931
Iberdomide purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2019 Feb 11;9(2):19. [Abstract]
lenalidomide-sensitive human papillomavirus (HMCL) cell lines (MM.1S, KMS11, XG1, and OPM2) in the presence of lenalidomide. The responses of these derived cell lines to the more potent immunomodulatory agent CC-220 (0-1000 nM, 5 days) were then examined.
Iberdomide purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2019 Feb 11;9(2):19. [Abstract]
The combination of SGC-CBP30 (0.2 and 0.4 μM, 5 days) and Lenalidomide (10 μM, 5 days) exerted substantial synergy in reducing the viability of myeloma XG1LenRes cells.
Iberdomide purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2019 Feb 11;9(2):19. [Abstract]
Immunoblotting assays detected the changes in IRF4, MYC, and STAT3 after treatment with Lenalidomide （10 μM） or SGC-CBP30 (0.2 and 0.4 μM) alone or in combination (day 3).
Iberdomide purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2019 Feb 11;9(2):19. [Abstract]
SGC-CBP30 (0.2 and 0.4 μM, 2 days) treatment also reduced autocrine IL-6 production in XG1LenRes cells, both in the absence and presence of Lenalidomide (10 μM, 2 days).
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Cell Rep Med
STAT3 couples activated tyrosine kinase signaling to the oncogenic core transcriptional regulatory circuitry of anaplastic large cell lymphoma. [Abstract]2024 Mar 19;5(3):101472. PMID: 38508140 -
Cell Chem Biol
A Cell-Based Target Engagement Assay for the Identification of Cereblon E3 Ubiquitin Ligase Ligands and Their Application in HDAC6 Degraders. [Abstract]2020 Jul 16;27(7):866-876.e8. PMID: 32413286 -
Elife
Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome. [Abstract]2018 Aug 1;7:e38430. PMID: 30067223
Iberdomide purchased from MedChemExpress. Usage Cited in: Elife. 2018 Aug 1;7:e38430. [Abstract]
SK-N-DZ cells were treated with 0.1 µM CC-220, 1 µM dBET57, 1 µM pomalidomide (3× biological replicates), or DMSO as a control (3× biological replicates) for 5 h. Protein abundance from each experiment was analyzed using TMT quantification mass spectrometry (see Materials and methods for details).
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J Proteome Res
2022 Aug 5;21(8):1842-1856. PMID: 35848491
Iberdomide purchased from MedChemExpress. Usage Cited in: J Proteome Res. 2022 Aug 5;21(8):1842-1856. [Abstract]
MM1S, HL60, and HCT116 cells were treated with 10 μM Lenalidomide, Pomalidomide, Avadomide, Iberdomide, CC-92480, CC-90009, CC-885, or DMSO as controls, respectively, and proteomics analysis was performed.
Iberdomide purchased from MedChemExpress. Usage Cited in: J Proteome Res. 2022 Aug 5;21(8):1842-1856. [Abstract]
Clustering of the protein abundance changes (drug/DMSO, log2) in three cell lines separated the compounds into two proteomic drug clusters: cluster1 (Lenalidomide, Pomalidomide, Avadomide, Iberdomide, CC-92480) that degrades C2H2 zinc finger proteins, and cluster2 (CC-90009 and CC-885) that degrades translation termination proteins GSPT1 and GSPT2.
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J Gastroenterol Hepatol
IKZF3 Promotes Gastric cancer Progression and Oxaliplatin Resistance via PI3K/AKT/mTOR Activation. [Abstract]2026 Mar 12. PMID: 41820205 -
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溶剤 & 溶解度
DMSO : 100 mg/mL (222.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.63 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.63 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
[1]. Chad C Bjorklund, et al. Iberdomide (CC-220) is a potent cereblon E3 ligase modulator with antitumor and immunostimulatory activities in lenalidomide- and pomalidomide-resistant multiple myeloma cells with dysregulated CRBN. Leukemia. 2020 Apr;34(4):1197-1201. [Content Brief]
[2]. Erin W Meermeier, et al. Tumor burden limits bispecific antibody efficacy through T cell exhaustion averted by concurrent cytotoxic therapy. Blood Cancer Discov. 2021 Jul;2(4):354-369. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2247 mL | 11.1235 mL | 22.2469 mL | 55.6174 mL |
| 5 mM | 0.4449 mL | 2.2247 mL | 4.4494 mL | 11.1235 mL | |
| 10 mM | 0.2225 mL | 1.1123 mL | 2.2247 mL | 5.5617 mL | |
| 15 mM | 0.1483 mL | 0.7416 mL | 1.4831 mL | 3.7078 mL | |
| 20 mM | 0.1112 mL | 0.5562 mL | 1.1123 mL | 2.7809 mL | |
| 25 mM | 0.0890 mL | 0.4449 mL | 0.8899 mL | 2.2247 mL | |
| 30 mM | 0.0742 mL | 0.3708 mL | 0.7416 mL | 1.8539 mL | |
| 40 mM | 0.0556 mL | 0.2781 mL | 0.5562 mL | 1.3904 mL | |
| 50 mM | 0.0445 mL | 0.2225 mL | 0.4449 mL | 1.1123 mL | |
| 60 mM | 0.0371 mL | 0.1854 mL | 0.3708 mL | 0.9270 mL | |
| 80 mM | 0.0278 mL | 0.1390 mL | 0.2781 mL | 0.6952 mL | |
| 100 mM | 0.0222 mL | 0.1112 mL | 0.2225 mL | 0.5562 mL |
Iberdomide 関連分類
HY-101291 関連分類
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