1. PROTAC Cytoskeleton
  2. Molecular Glues Integrin
  3. E7820

E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a molecular glue that induces the targeted degradation of splicing factor RBM39 by recruiting the E3 ubiquitin ligase CUL4-RBX1-DDB1-DCAF15 (CRL4DCAF15). E7820 is an angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. E7820 can be used for the study of acute myeloid leukemia (AML).

For research use only. We do not sell to patients.

CAS No. : 289483-69-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    E7820 purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2025 Aug 29;17(17):2846.  [Abstract]

    CCK8 assays showing reduced IC50 of lenvatinib after E7820 treatment in Hep3B-LR, Huh7-LR, and SNU449 cells.

    E7820 purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2025 Aug 29;17(17):2846.  [Abstract]

    Colony formation assays indicating enhanced inhibitory effect of lenvatinib by E7820.

    E7820 purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2025 Aug 29;17(17):2846.  [Abstract]

    CCK8 assays demonstrating E7820-promoted suppression of cell proliferation by lenvatinib.

    E7820 purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2025 Aug 29;17(17):2846.  [Abstract]

    Flow cytometry analysis of apoptosis after E7820 and lenvatinib treatment. The total apoptosis rate (sum of early and late apoptosis) is delineated by the yellow boxes.

    E7820 purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2025 Aug 29;17(17):2846.  [Abstract]

    Compared with those in the lenvatinib monotherapy group, the tumor growth rates of the mice in the lenvatinib combined with E7820 (5 mg/kg) treatment group were significantly lower, and the tumor weights were significantly lower.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a molecular glue that induces the targeted degradation of splicing factor RBM39 by recruiting the E3 ubiquitin ligase CUL4-RBX1-DDB1-DCAF15 (CRL4DCAF15). E7820 is an angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. E7820 can be used for the study of acute myeloid leukemia (AML)[1][2][3].

    In Vitro

    E7820 (ER68203-00) inhibits both bFGF- and VEGF-driven ube formation of human umbilical vascular endothelial cell (HUVEC) in a dose-dependent manner with IC50 of 0.20 and 0.24 μg/ml, respectively[1].
    E7820 inhibits proliferation of HUVEC induced by either bFGF or VEGF in serum-free medium (SFM). The IC50 values are 0.10 and 0.081 μg/ml, respectively. Antiproliferative activity of E7820 against both WiDr and LoVo cells is very weak compared with that against HUVEC. The values of IC50 were 29 and 15 μg/ml, respectively[1].

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

    In Vivo

    E7820 (ER68203-00) (50-200 mg/kg; p.o. ; twice daily for 14 days) delays the growth of WiDr cells inoculated s.c.[1].
    E7820 (200-400 mg/kg; p.o.;once daily for 4 days) potently inhibits WiDr-induced angiogenesis[1].

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

    Animal Model: Six-week-old female nude mice (KSN mice, WiDr-induced angiogenesis model) [1]
    Dosage: 50, 100, 200 mg/kg
    Administration: p.o. ; twice daily for 14 days from 2 days after inoculation of the tumor cells
    Result: The antitumor effect was dose-dependent at 50, 100, and 200 mg/kg, and the tumor growth rates were 52%, 46%, and 27%, respectively.
    Clinical Trial
    Molecular Weight

    336.37

    Formula

    C17H12N4O2S

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to light brown

    SMILES

    O=S(C1=CC(C#N)=CC=C1)(NC2=C(NC=C3C#N)C3=C(C)C=C2)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (297.29 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 2.9729 mL 14.8646 mL 29.7292 mL
    5 mM 0.5946 mL 2.9729 mL 5.9458 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.

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    • 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)

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    In Vivo:

    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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.43 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    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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    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.
    Purity & Documentation

    Purity: 99.26%

    References

    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 2.9729 mL 14.8646 mL 29.7292 mL 74.3229 mL
    5 mM 0.5946 mL 2.9729 mL 5.9458 mL 14.8646 mL
    10 mM 0.2973 mL 1.4865 mL 2.9729 mL 7.4323 mL
    15 mM 0.1982 mL 0.9910 mL 1.9819 mL 4.9549 mL
    20 mM 0.1486 mL 0.7432 mL 1.4865 mL 3.7161 mL
    25 mM 0.1189 mL 0.5946 mL 1.1892 mL 2.9729 mL
    30 mM 0.0991 mL 0.4955 mL 0.9910 mL 2.4774 mL
    40 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8581 mL
    50 mM 0.0595 mL 0.2973 mL 0.5946 mL 1.4865 mL
    60 mM 0.0495 mL 0.2477 mL 0.4955 mL 1.2387 mL
    80 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9290 mL
    100 mM 0.0297 mL 0.1486 mL 0.2973 mL 0.7432 mL
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    • 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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