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

Fimepinostat (Synonyms: CUDC-907)

Cat. No.: HY-13522 Purity: 99.95%
Handling Instructions

Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.

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

Fimepinostat Chemical Structure

Fimepinostat Chemical Structure

CAS No. : 1339928-25-4

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10 mM * 1 mL in Ethanol USD 157 In-stock
Estimated Time of Arrival: December 31
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5 mg USD 140 In-stock
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10 mg USD 190 In-stock
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50 mg USD 520 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Fimepinostat purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 May;40(5):677-688

    Aspc-1 and Capan-1 cells are collected for Western blotting with the indicated antibodies after treatment with CUDC-907 for 48 h.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.

    IC50 & Target

    PI3Kα

    19 nM (IC50)

    PI3Kδ

    39 nM (IC50)

    PI3Kβ

    54 nM (IC50)

    PI3Kγ

    311 nM (IC50)

    HDAC1

    1.7 nM (IC50)

    HDAC3

    1.8 nM (IC50)

    HDAC10

    2.8 nM (IC50)

    HDAC2

    5 nM (IC50)

    HDAC11

    5.4 nM (IC50)

    HDAC6

    27 nM (IC50)

    HDAC8

    191 nM (IC50)

    HDAC4

    409 nM (IC50)

    HDAC7

    426 nM (IC50)

    HDAC9

    554 nM (IC50)

    HDAC5

    674 nM (IC50)

    In Vitro

    Fimepinostat 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 LBH589 and greater than that of SAHA. Fimepinostat 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. Fimepinostat markedly induces p21 protein in H460, a non-small cell lung cancer (NSCLC) cell line. Fimepinostat 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. Fimepinostat induces caspase-3 and -7 activation in HCT-116 colon cancer cells in a dose-dependent manner. Fimepinostat potently inhibits the growth of cancer cells derived from both hematologic and solid tumors. Fimepinostat potently inhibits the proliferation of cells expressing either mutant or wild-type PI3K[1].

    In Vivo

    Oral administration of Fimepinostat 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, Fimepinostat achieves better efficacy than GDC-0941, SAHA, or a combination of these 2 compounds given at their maximal tolerated doses (MTD). Furthermore, Fimepinostat 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
    Molecular Weight

    508.55

    Formula

    C₂₃H₂₄N₈O₄S

    CAS No.

    1339928-25-4

    SMILES

    O=C(C1=CN=C(N(CC2=CC3=NC(C4=CC=C(OC)N=C4)=NC(N5CCOCC5)=C3S2)C)N=C1)NO

    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 : ≥ 50 mg/mL (98.32 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: 2.5 mg/mL (4.92 mM); Clear solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.92 mM); Clear solution

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

    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.,Fimepinostat) 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]

    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 Fimepinostat, 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

    Purity: 99.95%

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    Product name:
    Fimepinostat
    Cat. No.:
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