2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Epigenetics Cell Cycle/DNA Damage
  3. EGFR HDAC
  4. CUDC-101

CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

CUDC-101 Chemical Structure

CUDC-101 Chemical Structure

CAS No. : 1012054-59-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 9 publication(s) in Google Scholar

CUDC-101 Related Antibodies

Top Publications Citing Use of Products

    CUDC-101 purchased from MedChemExpress. Usage Cited in: Am J Cancer Res. 2018 Dec 1;8(12):2402-2418  [Abstract]

    Western analysis of protein levels of p-p53, cl-caspase3 and the ratio of bax/bcl-2 in the treatment of Germ or/and CUDC.

    CUDC-101 purchased from MedChemExpress. Usage Cited in: Am J Cancer Res. 2018 Dec 1;8(12):2402-2418  [Abstract]

    PANC-1 and MIA PaCa-2 cells are treated with CUDC-101 and/or gemcitabine for 48 h, and western blot analysis shows increased inhibition of the PI3K, p-Akt, p-S6, p-4EBP1 and p-Erk proteins.

    View All EGFR Isoform Specific Products:

    View All Isoforms
    EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

    View All HDAC Isoform Specific Products:

    View All Isoforms
    HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

    IC50 & Target[1]

    EGFR

    2.4 nM (IC50)

    HER2

    15.7 nM (IC50)

    HDAC

    4.4 nM (IC50)

    HDAC1

    4.5 nM (IC50)

    HDAC2

    12.6 nM (IC50)

    HDAC3

    9.1 nM (IC50)

    HDAC4

    13.2 nM (IC50)

    HDAC6

    5.1 nM (IC50)

    HDAC5

    11.4 nM (IC50)

    HDAC9

    67.2 nM (IC50)

    HDAC10

    26.1 nM (IC50)

    HDAC8

    79.8 nM (IC50)

    HDAC7

    373 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    BXPC-3 IC50
    0.27 μM
    Compound: 8, CDUC-101
    Antiproliferative activity against human BxPC3 cells after hrs by ATP content assay
    Antiproliferative activity against human BxPC3 cells after hrs by ATP content assay
    		[PMID: 20143778]
    CAPAN-1 IC50
    0.8 μM
    Compound: 8, CDUC-101
    Antiproliferative activity against human Capan1 cells after hrs by ATP content assay
    Antiproliferative activity against human Capan1 cells after hrs by ATP content assay
    		[PMID: 20143778]
    HCC827 IC50
    0.6 μM
    Compound: 8, CDUC-101
    Antiproliferative activity against human HCC827 cells after hrs by ATP content assay
    Antiproliferative activity against human HCC827 cells after hrs by ATP content assay
    		[PMID: 20143778]
    HeLa IC50
    4.2 nM
    Compound: 7; CUDC-101
    Inhibition of HDAC in human HeLa cell nuclear extract using COLOR DE LYS as substrate by fluorometric analysis
    Inhibition of HDAC in human HeLa cell nuclear extract using COLOR DE LYS as substrate by fluorometric analysis
    		[PMID: 27769671]
    HeLa IC50
    4.4 nM
    Compound: 7; CUDC-101
    Inhibition of HDAC (unknown origin) in human HeLa cell nuclear extract using Color de Lys as substrate
    Inhibition of HDAC (unknown origin) in human HeLa cell nuclear extract using Color de Lys as substrate
    		[PMID: 30418766]
    Hep 3B2 IC50
    0.23 μM
    Compound: 8, CDUC-101
    Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay
    Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay
    		[PMID: 20143778]
    HepG2 IC50
    0.13 μM
    Compound: 8, CDUC-101
    Antiproliferative activity against human HepG2 cells after hrs by ATP content assay
    Antiproliferative activity against human HepG2 cells after hrs by ATP content assay
    		[PMID: 20143778]
    MCF7 IC50
    0.55 μM
    Compound: CUDC-101
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by MTT assay
    		[PMID: 32320239]
    MCF7 IC50
    0.55 μM
    Compound: 8, CDUC-101
    Antiproliferative activity against human MCF7 cells after hrs by ATP content assay
    Antiproliferative activity against human MCF7 cells after hrs by ATP content assay
    		[PMID: 20143778]
    MDA-MB-231 IC50
    0.1 μM
    Compound: 8, CDUC-101
    Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay
    Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay
    		[PMID: 20143778]
    NCI-H358 IC50
    0.4 μM
    Compound: 8, CDUC-101
    Antiproliferative activity against human NCI-H358 cells after hrs by ATP content assay
    Antiproliferative activity against human NCI-H358 cells after hrs by ATP content assay
    		[PMID: 20143778]
    NCI-H460 IC50
    0.7 μM
    Compound: 8, CDUC-101
    Antiproliferative activity against human H460 cells after hrs by ATP content assay
    Antiproliferative activity against human H460 cells after hrs by ATP content assay
    		[PMID: 20143778]
    SK-BR-3 IC50
    0.04 μM
    Compound: 8, CDUC-101
    Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay
    Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay
    		[PMID: 20143778]
    SK-HEP1 IC50
    0.22 μM
    Compound: 8, CDUC-101
    Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay
    Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay
    		[PMID: 20143778]
    In Vitro

    CUDC-101 inhibits both class I and class II HDACs, but not class III, Sir-type HDACs. CUDC-101 displays broad antiproliferative activity in many human cancer cell types. CUDC-101 is a potent and selective HDAC, EGFR, and HER2 inhibitor with only weak inhibition of the following protein kinases (IC50): KDR (VEGFR2) (849 nM), Src (11000 nM), Lyn (840 nM), Lck (5910 nM), Abl-1 (2890 nM), FGFR-2 (3430 nM), Flt-3 (1500 nM), and Ret (3200 nM)[1].
    CUDC-101 (300 nM) inhibits both the full length AR (flAR) and the AR variant AR-V7[2].
    CUDC-101 is the most active agent in all three ATC cell lines screened for inhibitors of EGFR and HDACs, with half-maximal inhibitory concentration (IC50) at 0.15 μM for 8505c, and 1.66 μM for both C-643 and SW-1736 cells. CUDC-101 inhibits cancer cell migration and modulates epithelial-mesenchymal transition marker expression in ATC cells. CUDC-101 also inhibits HDAC and MAPK pathway, induces p21, and decreases survivin and XIAP expression in ATC cells[3].
    CUDC-101 (1 μM) increases the acetylation of p53 and α-tubulin, nonhistone substrates of HDAC, in treated cancer cells. CUDC-101 modulates RTK activity and expression and exhibits immediate and stable inhibition of RTK and downstream Akt signaling[4].

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

    CUDC-101 Related Antibodies
    In Vivo

    CUDC-101 (120 mg/kg, iv, daily) induces tumor regression in the Hep-G2 liver cancer model and is more efficacious than erlotinib at its maximum tolerated dose (MTD). In the erlotinib-resistant A549 NSCLC xenograft model, CUDC-101 (120 mg/kg) shows potent inhibition of tumor growth. In the erlotinib-sensitive H358 NSCLC models, CUDC-101 (15, 30, 60 mg/kg, i.v.) inhibits tumor growth in a dose-dependent manner. CUDC-101 (120 mg/kg) causes significant tumor regression in the lapatinib-resistant, HER2-negative, EGFR-overexpressing MDA-MB-468 breast cancer model and the EGFR-overexpressing CAL-27 head and neck squamous cell carcinoma (HNSCC) model. CUDC-101 (120 mg/kg) also inhibits tumor growth in the K-ras mutant HCT116 colorectal and EGFR/HER2 (neu)-expressing HPAC pancreatic cancer models[1].
    In an in vivo mouse model of metastatic ATC, CUDC-101 inhibits tumor growth and metastases, and significantly prolongs survival[3].
    CUDC-101 (120 mg/kg) is effective against a broad range of tumor types in xenograft models[4].

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

    434.49

    Formula

    C24H26N4O4
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    C#CC1=CC=CC(NC2=NC=NC3=CC(OC)=C(C=C23)OCCCCCCC(NO)=O)=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (57.54 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 2.3015 mL 11.5077 mL 23.0155 mL
    5 mM 0.4603 mL 2.3015 mL 4.6031 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.79 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 (4.79 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 16.67 mg/mL (38.37 mM); Suspended solution; Need ultrasonic

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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: 99.05%

    SDS (393 KB)

    COA (244 KB) HNMR (257 KB) RP-HPLC (256 KB) LCMS (106 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    The activities of Class I and II HDACs are assessed using the Biomol Color de Lys system. Briefly, HeLa cell nuclear extracts are used as a source of HDACs. Different concentrations of drugs are added to HeLa cell nuclear extracts in the presence of a colorimetric artificial substrate. Developer is added at the end of the assay and enzyme activity is measured in the Wallac Victor II 1420 microplate reader at 405 nM.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    Cancer cell lines are plated at 5000 to 10 000 cells per well in 96-well flat-bottomed plates with varying concentrations of compounds. The cells are incubated with compounds for 72 h in the presence of 0.5% of fetal bovine serum. Growth inhibition is assessed by an adenosine triphosphate (ATP) content assay using the Perkin-Elmer ATPlite kit.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Four- to six-week-old female athymic mice (nude nu/nu CD-1) are inoculated subcutaneously into the right hind flank region with 1 to 5×106 cells in a medium suspension of 100−200 μL. For orthotopic implantation of breast cancer cells, a cell suspension in 100 μL of medium is injected directly into the mammary fat pads through a 27G needle. Different doses of CUDC-101, standard anticancer agents and vehicle are administered orally, intraperitoneally, or via tail vein injection as indicated.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3015 mL 11.5077 mL 23.0155 mL 57.5387 mL
    5 mM 0.4603 mL 2.3015 mL 4.6031 mL 11.5077 mL
    10 mM 0.2302 mL 1.1508 mL 2.3015 mL 5.7539 mL
    15 mM 0.1534 mL 0.7672 mL 1.5344 mL 3.8359 mL
    20 mM 0.1151 mL 0.5754 mL 1.1508 mL 2.8769 mL
    25 mM 0.0921 mL 0.4603 mL 0.9206 mL 2.3015 mL
    30 mM 0.0767 mL 0.3836 mL 0.7672 mL 1.9180 mL
    40 mM 0.0575 mL 0.2877 mL 0.5754 mL 1.4385 mL
    50 mM 0.0460 mL 0.2302 mL 0.4603 mL 1.1508 mL
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    CUDC-101 Related Classifications

    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:

    CUDC-1011012054-59-9CUDC101CUDC 101EGFRHDACEpidermal growth factor receptorErbB-1HER1Histone deacetylasesInhibitorinhibitorinhibit

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