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

CUDC-101 

Cat. No.: HY-10223 Purity: 99.02%
Handling Instructions

CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4, 2.4, and 15.7 nM, respectively.

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 USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 102 In-stock
Estimated Time of Arrival: December 31
50 mg USD 348 In-stock
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100 mg USD 576 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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 MCE. Usage Cited in: Am J Cancer Res. 2018 Dec 1;8(12):2402-2418

    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.
    • 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.

    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)

    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].

    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].

    Clinical Trial
    Molecular Weight

    434.49

    Formula

    C₂₄H₂₆N₄O₄

    CAS No.

    1012054-59-9

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (57.54 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM 0.2302 mL 1.1508 mL 2.3015 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (5.75 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.02%

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    Product Name:
    CUDC-101
    Cat. No.:
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