2. PROTAC Apoptosis
  3. Ligands for E3 Ligase Apoptosis Molecular Glues
  4. Iberdomide

Iberdomide  (Synonyms: CC-220)

製品番号: HY-101291 純度: 99.54%
COA 取扱説明書 Technical Support

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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CAS 番号 : 1323403-33-3

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 在庫あり
Solution
10 mM * 1 mL in DMSO USD 132 在庫あり
Solid
2 mg $70 在庫あり
5 mg $120 在庫あり
10 mg $210 在庫あり
25 mg $420 在庫あり
50 mg $650 在庫あり
100 mg $980 在庫あり
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カスタマーレビュー

Based on 11 publication(s) in Google Scholar

Other Forms of Iberdomide:

Iberdomide 関連抗体

Top Publications Citing Use of Products

    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.

    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.

    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.

    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).

    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).

    Ligands for E3 Ligase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    von Hippel-Lindau (VHL) MDM2 Cereblon IAP KLHDC2 Fbxo3 RNF4 DCAF11 DCAF1 UHRF1 TRIM21 NEURL1B KLHL41

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    • 純度とドキュメンテーション

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    製品説明

    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[1][2].

    IC50 & Target

    Cereblon

     

    Cellular Effect
    Cell Line Type Value Description References
    MM1.S IC50
    13 nM
    Compound: CC-220
    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
    		[PMID: 31125896]
    MV4-11 IC50
    > 20000 nM
    Compound: CC-220
    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
    		[PMID: 31125896]
    体外実験

    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.

    Iberdomide 関連抗体
    体内実験

    Iberdomide (CC-220; 10 mg/kg; oral gavage) after 6 or 24 hours causes higher hCRBN expression in hC343 splenocytes correlated to deeper IKZF1/3 downregulation in WT (C57BL/6), hC123, or-343, (representing two different transgenic founder lines expressing hCRBN) and mCrbn-/- mice[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    449.50

    分子式

    C25H27N3O5
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@@H](N(CC1=C2C=CC=C1OCC3=CC=C(CN4CCOCC4)C=C3)C2=O)CC5)NC5=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

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    濃度 （終了）

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    体積 （終了）

    V2

    体内:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    (per animal)

    g

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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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    % 
    +
    %
    Tween-80 +
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    純度とドキュメンテーション

    純度: 99.54%

    COA (252 KB) HNMR (259 KB) LCMS (93 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [1]

    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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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
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    Iberdomide Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Iberdomide1323403-33-3CC-220CC220CC 220Ligands for E3 LigaseApoptosisMolecular GluesE3 ligase-recruiting MoietyorallycereblonCRBNE3ligaseCELMoDThalidomidemultiplemyelomaEJMH929KMS11KMS128MKMS12PEMM1.SMM1.RRPM-8226U266G0/G1sub-G1Inhibitorinhibitorinhibit

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