1. Epigenetics
    Cell Cycle/DNA Damage
    PI3K/Akt/mTOR
  2. HDAC
    PI3K

CUDC-907 

Cat. No.: HY-13522 Purity: 98.19%
Data Sheet SDS Handling Instructions

CUDC-907 potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with IC50 of 1.7/5.0/1.8/2.8 nM and 19/54/39 nM for HDAC1/2/3/10 and PI3Kα/β/δ, respectively.

For research use only. We do not sell to patients.
CUDC-907 Chemical Structure

CUDC-907 Chemical Structure

CAS No. : 1339928-25-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO $168 In-stock
2 mg $120 In-stock
5 mg $150 In-stock
10 mg $230 In-stock
50 mg $620 In-stock
100 mg   Get quote  
200 mg   Get quote  

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    CUDC-907 purchased from MCE. Usage Cited in: ACS Med Chem Lett. 2015 Jun 22;6(8):948-52.

    Combination treatment. (a) Comparison of AZD-8055 and ABT-263 treatment in all cell lines. Red indicates sensitivity, while blue indicates resistance. (b) Depiction of synergism where the values shown are excess over Bliss Independence, a prediction of inhibition without synergism. Increased synergism is evident by an increased number, shown in red, while negative numbers in blue represent an antagonistic effect.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    CUDC-907 potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with IC50 of 1.7/5.0/1.8/2.8 nM and 19/54/39 nM for HDAC1/2/3/10 and PI3Kα/β/δ, respectively.

    IC50 & Target

    IC50: 1.7/5.0/1.8/2.8 nM (HDAC1/2/3/10), 19/54/39 nM (PI3Kα/β/δ)[1]

    In Vitro

    CUDC-907 is a potent pan-inhibitor of HDAC classes I and II enzymes and observed that its potency against class I HDACs is similar to that of panobinostat and greater than that of vorinostat. CUDC-907 is also a potent inhibitor of class I PI3K kinases with an IC50 of 19, 54, and 39 nM for PI3Kα, PI3Kβ, and PI3Kδ, respectively. CUDC-907 markedly induces p21 protein in H460, a non-small cell lung cancer (NSCLC) cell line. CUDC-907 causes the reduction of both p-STAT3 (Y-705) and p-SRC in RPMI-8226 multiple myeloma cells and reduces both phosphorylated and total protein levels of MET and EGFR as well as HER2 and HER3 in H1975 NSCLC cells and BT-474 breast cancer cells, respectively. CUDC-907 induces caspase-3 and -7 activation in HCT-116 colon cancer cells in a dose-dependent manner. CUDC-907 potently inhibits the growth of cancer cells derived from both hematologic and solid tumors. CUDC-907 potently inhibits the proliferation of cells expressing either mutant or wild-type PI3K[1].

    In Vivo

    Oral administration of CUDC-907 inhibits growth of the Daudi cancer cell xenografts in a dose-dependent manner. Tumor stasis is observed at 100 mg/kg in this model without obvious toxicity. Importantly, in the same model, CUDC-907 achieves better efficacy than GDC-0941, Vorinostat, or a combination of these 2 compounds given at their maximal tolerated doses (MTD). Furthermore, CUDC-907 causes tumor regression or stasis after intravenous (50 mg/kg) or oral administration (100 mg/kg) in a xenograft tumor model of SU-DHL4 diffuse large B-cell lymphoma (DLBCL) and causes tumor stasis in KRAS-mutant A549 NSCLC cell xenografts[1].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT02307240 Curis, Inc. NUT Midline Carcinoma|Breast Cancer|Solid Tumors November 2014 Phase 1
    NCT01742988 Curis, Inc.|The Leukemia and Lymphoma Society Multiple Myeloma|Lymphoma December 2012 Phase 1
    NCT02674750 Curis, Inc. Relapsed and/or Refractory Diffuse Large B-cell Lymphoma Including With Myc Alterations January 2016 Phase 2
    NCT02909777 Dana-Farber Cancer Institute|Curis, Inc. Lymphoma|Neuroblastoma|Brain Tumor|Solid Tumor October 2016 Phase 1
    NCT03002623 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Thyroid Neoplasms|Poorly Differentiated and Undifferentiated Thyroid Cancer|Differentiated Thyroid Cancer December 16, 2016 Phase 2
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 1.9664 mL 9.8319 mL 19.6637 mL
    5 mM 0.3933 mL 1.9664 mL 3.9328 mL
    10 mM 0.1966 mL 0.9832 mL 1.9664 mL
    Kinase Assay
    [1]

    The activities of classes I and II HDACs are measured using the Color-de-Lys assay system. The activity of PI3K is measured using the ADP-Glo luminescent kinase assay. Recombinant PI3K protein, a complex of N-terminal GST-tagged recombinant full-length human p110 and untagged recombinant full-length human p85, is coexpressed in a baculovirus-infected Sf9 cell expression system[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    CUDC-907 is dissolved in DMSO and stored (-80°C), and then diluted with appropriate medium before use[1].

    Human cancer cell lines are plated at densities of 5,000 to 10,000 per well in 96-well flat-bottomed plates with the recommended culture medium. The cells are then incubated with compounds (e.g.,CUDC-907) at various concentrations for 72 hours in culture medium supplemented with 0.5% (v/v) FBS. Growth inhibition is assessed by assay of cellular ATP content using the Perkin-Elmer ATPlite kit[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    CUDC-907 is formulated in 30% Captisol (Mice)[1].

    Mice[1]
    Six- to 8-week-old female athymic (nude nu/nu CD-1) or severe combined immunodeficient (SCID) mice obtained from Charles River Laboratories are injected subcutaneously with 3 to 20×106 cells in a medium suspension of 100 to 200 μL into the right hind flank region. Varying doses of CUDC-907, standard anticancer agents, or vehicle are administered orally or via tail vein injection as indicated. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    508.55

    Formula

    C₂₃H₂₄N₈O₄S

    CAS No.

    1339928-25-4

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    CUDC-907
    Cat. No.:
    HY-13522
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