| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Iberdomide (also known as CC-220) is a novel and potent cereblon (CRBN) modulator with an IC50 of 60 nM and can be potentially used for the treatment of systemic lupus erythematosus. Iberdomide significantly reduced Ikaros and Aiolos protein levels in B cells, T cells and monocytes. In SLE PBMC cultures, iberdomide inhibited anti-dsDNA and anti-phospholipid autoantibody production (IC50 ≈10 nM).
| ln Vitro |
A panel of multiple myeloma (MM) cell lines (EJM, H929, KMS11, KMS128M, KMS12PE, MM1.S, MM1.R, RPM-8226, U266 cells) showed antiproliferative effects across a range of concentrations when iberdomide (CC-220; 0.01, 0.1, 1, 10 μM; 72-96 hrs) was administered[1].
In all MM cell lines, iberdomide (0.1 μM; 96 hrs) causes apoptosis[1]. On H929 cells, imiberdomide (0.1 μM; 24, 48, and 72 hours) causes time-dependent increases in the G0/G1 and sub-G1 cell cycle fractions[1]. In the KMS12BM line, iberdomide causes rapid Aiolos depletion[1]. In two of the Pomalidomide-resistant (PR) lines with cereblon mutations (EJM/PR and H929/PR), imiberdomide (0.1 μM) exhibits some anti-proliferative activity in addition to decreased levels of cereblon protein[1]. Both parental MM1.S cells and MM1.S/PR cells are equally susceptible to PBMC-mediated killing when exposed to iberdomide (0.1-1000 nM) for 72 hours[1]. |
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| ln Vivo |
Higher hCRBN expression in hC343 splenocytes following 6 or 24 hours of iberdomide (CC-220; 10 mg/kg; oral gavage) is correlated with deeper IKZF1/3 downregulation in WT (C57BL/6), hC123 or-343 (representing two distinct transgenic founder lines expressing hCRBN), and mCrbn-/- mice[2].
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| Enzyme Assay |
DMSO is used to dissolve iberdomide. The assay uses 20 mM HEPES pH 7, 150 mM NaCl, 0.005% Tween-20 assay buffer, 60 nM 6Xhis-tagged CRBN-DDB1, 30 nM cy5-conjugated cereblon modulator, and 3 nM LanthaScreen Eu-anti-His Tag antibody. The ratio of FRET to non-FRET emission is used to calculate FRET efficiency. FRET is observed by exciting at 340 nm and monitoring emission at 615 nm and 665 nm. Prior to scanning, the DMSO carrier or the competing cereblon modulating compound (iberdomide) is titrated and incubated for ten minutes[1].
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| References |
| Molecular Formula |
C25H27N3O5
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|---|---|
| Molecular Weight |
449.4990
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| Exact Mass |
449.20
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| Elemental Analysis |
449.500
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| CAS # |
1323403-33-3
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| Related CAS # |
1560678-63-8 (HCl);1323403-33-3;
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| Appearance |
Solid powder
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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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| InChi Key |
IXZOHGPZAQLIBH-NRFANRHFSA-N
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| InChi Code |
InChI=1S/C25H27N3O5/c29-23-9-8-21(24(30)26-23)28-15-20-19(25(28)31)2-1-3-22(20)33-16-18-6-4-17(5-7-18)14-27-10-12-32-13-11-27/h1-7,21H,8-16H2,(H,26,29,30)/t21-/m0/s1
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| Chemical Name |
(S)-3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione
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| Synonyms |
CC-220; CC220; CC 220.
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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 : 90~125 mg/mL ( 200.22~278.09 mM )
Ethanol : ~5 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.63 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2247 mL | 11.1235 mL | 22.2469 mL | |
| 5 mM | 0.4449 mL | 2.2247 mL | 4.4494 mL | |
| 10 mM | 0.2225 mL | 1.1123 mL | 2.2247 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04564703 | Active, not recruiting | Drug: Iberdomide | Multiple Myeloma |
European Myeloma Network | February 22, 2021 | Phase 2 |
| NCT04392037 | Active, not recruiting | Drug: Iberdomide plus low-dose cyclophosphamide dexamethasone |
Multiple Myeloma |
Amsterdam UMC location VUmc |
February 17, 2021 | Phase 2 |
| NCT04933747 | Completed | Drug: Iberdomide | Renal Insufficiency |
Celgene | August 12, 2021 | Phase 1 |
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