1. PROTAC
  2. Molecular Glues Ligands for E3 Ligase
  3. CC-885

CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity. CC-885 is also a known degrader of GSPT1, inhibiting protein translation.

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CAS 番号 : 1010100-07-8

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10 mg $210 在庫あり
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カスタマーレビュー

Based on 18 publication(s) in Google Scholar

Other Forms of CC-885:

Top Publications Citing Use of Products

    CC-885 purchased from MedChemExpress. Usage Cited in: Cell. 2023 Jul 20;186(15):3227-3244.e20.  [Abstract]

    Immunoblot analysis of eRF3 upon treatment of HEK293T cells with CC-885 (10 nM) and G418 (20 μg/mL) for 4 h to induce readthrough (n = 3).

    CC-885 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2024 Sep;20(9):1227-1236.  [Abstract]

    GSPT1, VCL and ETF1 proteins in 293T cells treated with CC-885 (1 μM; 0.5-24 h) over the indicated time course were analyzed by immunoblotting.

    CC-885 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Dec 19;14(1):8437.  [Abstract]

    Degradation of neo-substrates by CC-885 (0.00001-10000 nM) in MM.1 S cells after 16 h treatment. Graph bars represent mean values ± SD. n = 3 independent biological replicates. Immunoblot experiment was performed to check protein level. Quantitative protein analysis was performed by software Image J. Source data are provided as a Source Data file.

    CC-885 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Dec 19;14(1):8437.  [Abstract]

    Western blot using lysates from Ba/F3 cells overexpressing Crbn constructs with combinations of humanization mutations E152D, V380E, and I391V as indicated. Protein lysates were harvested following 6 hours of treatment with 1 μM CC-885.

    CC-885 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Sep 10;13(1):5324.  [Abstract]

    RT-qPCR data showing expression of COL1A1 and COL3A1 upon treatment of LX2 cells (left panel) or EMS404 cells (right panel) with increasing concentrations of CC-885 (0.001-1 μM) or vehicle for 24h (n=3 biologically independent experiments). Log2 FC between drug and vehicle-treated cells are shown. The bar graph shows means ±SD.

    CC-885 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2022 Aug 15;132(16):e153514.  [Abstract]

    Cell viability in MOLM13 cells expressing GSPT1-ETF1Δ (drug sensitive and drug resistant; G575N). For all CellTiter-Glo luminescent assays, cell viability was assessed 72 hours after treatment with CC-885 (0.001-1 μM, graphs represent combined data from 3 biological replicates performed in technical triplicate; symbols represent mean ± SEM).
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    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity. CC-885 is also a known degrader of GSPT1, inhibiting protein translation.

    IC50 & Target

    Cereblon

     

    Cellular Effect
    Cell Line Type Value Description References
    BE(2)-C EC50
    < 5 nM
    Compound: CC-885
    Antiproliferative activity against wild type human BE2C cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
    Antiproliferative activity against wild type human BE2C cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
    [PMID: 38608634]
    HK-2 IC50
    0.002 μM
    Compound: 154; CC-885
    Downregulation of BNIP3 expression in human HK-2 cells incubated for 6 hrs by Western blot analysis
    Downregulation of BNIP3 expression in human HK-2 cells incubated for 6 hrs by Western blot analysis
    [PMID: 38295689]
    HL-60 IC50
    0.003 μM
    Compound: 3; CC-885
    Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    [PMID: 33591756]
    JeKo-1 IC50
    1.2 nM
    Compound: CC-885
    Antiproliferative activity against human JeKo1 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    Antiproliferative activity against human JeKo1 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    [PMID: 31125896]
    KG-1 IC50
    0.007 μM
    Compound: 3; CC-885
    Antiproliferative activity against human KG-1 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    Antiproliferative activity against human KG-1 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    [PMID: 33591756]
    KG-1a IC50
    0.008 μM
    Compound: 3; CC-885
    Antiproliferative activity against human KG-1a cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    Antiproliferative activity against human KG-1a cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    [PMID: 33591756]
    Kasumi 1 IC50
    0.01 μM
    Compound: 3; CC-885
    Antiproliferative activity against human Kasumi 1 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    Antiproliferative activity against human Kasumi 1 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    [PMID: 33591756]
    Kasumi 1 IC50
    0.8 nM
    Compound: CC-885
    Antiproliferative activity against human Kasumi-1 cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    Antiproliferative activity against human Kasumi-1 cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    [PMID: 31125896]
    MCF-10A IC50
    0.005 μM
    Compound: CC-885
    Cytotoxicity against human MCF10A cells after 72 hrs by MTS assay
    Cytotoxicity against human MCF10A cells after 72 hrs by MTS assay
    [PMID: 29795767]
    MM1.S IC50
    0.3 nM
    Compound: CC-885
    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]
    MOLM-13 IC50
    0.008 μM
    Compound: 3; CC-885
    Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    [PMID: 33591756]
    MOLT-4 EC50
    < 1 nM
    Compound: CC-885
    Antiproliferative activity against wild type human MOLT-4 cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
    Antiproliferative activity against wild type human MOLT-4 cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
    [PMID: 38608634]
    MV4-11 EC50
    < 1 nM
    Compound: CC-885
    Antiproliferative activity against wild type human MV4-11 cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
    Antiproliferative activity against wild type human MV4-11 cells assessed as reduction in cell viability measured after 3 days by ATP-dependent luminescence assay
    [PMID: 38608634]
    MV4-11 IC50
    0.005 μM
    Compound: 3; CC-885
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    [PMID: 33591756]
    MV4-11 IC50
    0.2 nM
    Compound: CC-885
    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]
    MV4-11 IC50
    0.3 nM
    Compound: CC-885
    Antiproliferative activity against human MV411 cells after 72 hrs by MTS assay
    Antiproliferative activity against human MV411 cells after 72 hrs by MTS assay
    [PMID: 29795767]
    NB-4 IC50
    0.002 μM
    Compound: 3; CC-885
    Antiproliferative activity against human NB4 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    Antiproliferative activity against human NB4 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    [PMID: 33591756]
    OCI-AML-3 IC50
    0.073 μM
    Compound: 3; CC-885
    Antiproliferative activity against human OCI-AML3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    Antiproliferative activity against human OCI-AML3 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    [PMID: 33591756]
    OCI-AML2 IC50
    0.021 μM
    Compound: 3; CC-885
    Antiproliferative activity against human OCI-AML2 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    Antiproliferative activity against human OCI-AML2 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    [PMID: 33591756]
    PBMC IC50
    0.3 nM
    Compound: CC-885
    Cytotoxicity against human PBMC cells by CellTiter96 Aqueous non-radioactive cell proliferation assay
    Cytotoxicity against human PBMC cells by CellTiter96 Aqueous non-radioactive cell proliferation assay
    [PMID: 31125896]
    PBMC IC50
    > 5 μM
    Compound: 3; CC-885
    Cytotoxicity against PBMC (unknown origin)
    Cytotoxicity against PBMC (unknown origin)
    [PMID: 32130004]
    RPMI-8226 IC50
    5.5 nM
    Compound: CC-885
    Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    [PMID: 31125896]
    Raji IC50
    20.4 nM
    Compound: CC-885
    Antiproliferative activity against human Raji cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    Antiproliferative activity against human Raji cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    [PMID: 31125896]
    SNU-C4 CC50
    440 nM
    Compound: CC-885
    Cytotoxicity against PXR knock in human SNU-C4 cells measured after 72 hrs by celltiter-glo assay
    Cytotoxicity against PXR knock in human SNU-C4 cells measured after 72 hrs by celltiter-glo assay
    [PMID: 35978691]
    THLE-2 IC50
    0.011 μM
    Compound: 3; CC-885
    Cytotoxicity against human THLE-2 cells assessed as cell viability incubated for 72 hrs by cell titer glo assay
    Cytotoxicity against human THLE-2 cells assessed as cell viability incubated for 72 hrs by cell titer glo assay
    [PMID: 33591756]
    THP-1 IC50
    1.5 nM
    Compound: CC-885
    Antiproliferative activity against human THP1 cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    Antiproliferative activity against human THP1 cells measured after 168 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    [PMID: 31125896]
    U-266 IC50
    2 nM
    Compound: CC-885
    Antiproliferative activity against human U266 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    Antiproliferative activity against human U266 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    [PMID: 31125896]
    U-937 IC50
    0.011 μM
    Compound: 3; CC-885
    Antiproliferative activity against human U937 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    Antiproliferative activity against human U937 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
    [PMID: 33591756]
    WI-38 IC50
    > 20 μM
    Compound: CC-885
    Cytotoxicity against human WI38 cells after 72 hrs by MTS assay
    Cytotoxicity against human WI38 cells after 72 hrs by MTS assay
    [PMID: 29795767]
    Z-138 IC50
    0.4 nM
    Compound: CC-885
    Antiproliferative activity against human Z138 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    Antiproliferative activity against human Z138 cells measured after 72 hrs by CellTiter96 Aqueous non-radioactive cell proliferation assay
    [PMID: 31125896]
    体外実験

    Acute myeloblatlic leukemia (AML) cell lines, human liver epithelial cell line (THLE-2) and human peripheral blood mononuclear cells (PBMC) are treated with varying concentrations of CC-885, with IC50s of 10×-6-1 μM. The effect of CC-885 on cell proliferation in AML cell lines, THLE-2 and human PBMC is more powerful than Lenalidomide and Pomalidomide with IC50s>10 μM. To address whether the cereblon-dependent degradation of GSPT1 is responsible for the cytotoxic effects of CC-885, a GSPT1 mutant that retains its normal function, but loses CC-885-dependent cereblon binding, is used to distinguish the role of GSPT1 from that of other substrates. CC-885 is tested in 293T HEK cells stably expressing the CC-885-sensitive or -resistant GSPT1 variants. Overexpression of a resistant variant GSPT1Δ(1–138)/(G575N) completely abrogate the CC-885-induced anti-proliferation, whereas overexpression of a CC-885-sensitive variant GSPT1Δ(1-138) only confer partial protection. Similar results are obtained in AML cell lines[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    440.88

    分子式

    C22H21ClN4O4

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NCC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2)=O)C=C1)NC4=CC=C(C)C(Cl)=C4

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 66.67 mg/mL (151.22 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 2.2682 mL 11.3410 mL 22.6819 mL
    5 mM 0.4536 mL 2.2682 mL 4.5364 mL
    10 mM 0.2268 mL 1.1341 mL 2.2682 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

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    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始)

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    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: 2.25 mg/mL (5.10 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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% Corn Oil

      Solubility: ≥ 2.25 mg/mL (5.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
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    Please enter your animal formula composition:
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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: 99.26%

    参考文献
    細胞実験
    [1]

    Human cancer cell lines cultured in the growth medium are seeded into black 384-well plates containing DMSO or test compounds such as CC-885 (10×-6-1 μM). The seeding density for each cell line is optimized to allow the cell growth in the linear range during a 3-day culture period. To test the compound effect on cell proliferation in acute myeloid leukaemia (AML) cell lines, 5,000 to 10,000 cells per well in 200 μl complete culture media are seeded into black 96-well plates containing DMSO or test compounds such as CC-885. After 48 or 72 h, cell proliferation is assessed using the CellTiter-Glo (CTG) Luminescent Cell Viability Assay[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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2682 mL 11.3410 mL 22.6819 mL 56.7048 mL
    5 mM 0.4536 mL 2.2682 mL 4.5364 mL 11.3410 mL
    10 mM 0.2268 mL 1.1341 mL 2.2682 mL 5.6705 mL
    15 mM 0.1512 mL 0.7561 mL 1.5121 mL 3.7803 mL
    20 mM 0.1134 mL 0.5670 mL 1.1341 mL 2.8352 mL
    25 mM 0.0907 mL 0.4536 mL 0.9073 mL 2.2682 mL
    30 mM 0.0756 mL 0.3780 mL 0.7561 mL 1.8902 mL
    40 mM 0.0567 mL 0.2835 mL 0.5670 mL 1.4176 mL
    50 mM 0.0454 mL 0.2268 mL 0.4536 mL 1.1341 mL
    60 mM 0.0378 mL 0.1890 mL 0.3780 mL 0.9451 mL
    80 mM 0.0284 mL 0.1418 mL 0.2835 mL 0.7088 mL
    100 mM 0.0227 mL 0.1134 mL 0.2268 mL 0.5670 mL
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    • Molarity Calculator

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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

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    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.

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    Inquiry Information

    製品名:
    CC-885
    製品番号:
    HY-101488
    数量:
    MCE 日本正規代理店: