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    Fimepinostat (CUDC907)
    Fimepinostat (CUDC907)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0132
    CAS #: 1339928-25-4Purity ≥98%

    Description: Fimepinostat (also known as CUDC-907) is a potent, orally bioavailable, and small molecule dual inhibitor of PI3K and HDAC (PI3Kα and HDAC1/2/3/10) with potential anticancer activity. It inhibits PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. Fimepinostat is under investigation by Curis in a Phase 2 clinical trial to treat patients with relapsed, refractory diffuse large B-cell lymphoma (DLBCL), and a Phase 1 trial in patients with solid tumors.

    References:Clin Cancer Res. 2012 Aug 1;18(15):4104-13; Am J Transl Res. 2011 Feb;3(2):166-79.


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    Molecular Weight (MW)

    508.55

    Formula

    C23H24N8O4S

    CAS No.

    1339928-25-4

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 102 mg/mL (200.6 mM)

    Water:<1 mg/mL

    Ethanol: <1 mg/mL

    Synonyms

    CUDC907; CUDC 907; CUDC-907

    Chemical Name

    N-hydroxy-2-[[2-(6-methoxypyridin-3-yl)-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl-methylamino]pyrimidine-5-carboxamide


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    In Vitro

    Kinase Assay: 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

     

    Cell Assay: CUDC-907 inhibits other PI3K isoforms such as PI3Kβ, PI3Kγ, PI3Kδ, PI3KɑH1047R and PI3KɑE545K with IC50 of 54 nM, 311 nM, 39 nM, 73 nM and 62 nM, respectively. Moreover, CUDC-907 also prevents HDAC subtypes HDAC8, HDAC6 and HDAC11 with IC50 of 191 nM, 27 nM and 5.4 nM, respectively. In addition, CUDC-907 suppresses other types of HDAC enzymatic activity with lower potency. CUDC-907 inhibits the growth of a series of B cell lymphoma such as Granta 519, DOHH2, RL, Pfeiffer, SuDHL4, Daudi and Raji with IC50 of 7 nM, 1 nM, 2 nM, 4 nM, 3 nM, 15 nM and 9 nM, respectively. CUDC-907 also blocks the proliferation of Myeloma including RPMI8226, OPM-2 and ARH77 with IC50 of 2 nM, 1 nM and 5 nM, respectively. CUDC-907 displays greater anti-tumor activity in multiple myeloma and B cell lymphoma.

    In Vivo

    CUDC-907 has a long half-life in murine tumors. CUDC-907 induces apoptosis and inhibits cancer cell proliferation in xenograft tumors. In efficacy studies in NHL and MM models, CUDC-907 is more efficacious than either a single-agent PI3K or HDAC inhibitor reference compound or a combination of the two agents given at maximally tolerated doses (MTD). Furthermore, CUDC-907 is more efficacious than the PI3Kδ-selective inhibitor CAL-101 when dosed at MTD doses.

    Animal model

    NHL and MM models in mice

    Formulation & Dosage

    100 mg/kg; oral administration

    References

     2012 Aug 1;18(15):4104-13; Bao R,et al. 2012, AACR Poster # 3744


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Fimepinostat (CUDC-907)

    CUDC-907 design and its potency against PI3K and HDAC.  Clin Cancer Res. 2012 Aug 1;18(15):4104-13. 

    Fimepinostat (CUDC-907)

    CUDC-907 evades drug resistance and induces apoptosis and G2–M phase cell-cycle arrest. Clin Cancer Res. 2012 Aug 1;18(15):4104-13. 

    Fimepinostat (CUDC-907)

    CUDC-907 durably suppresses activation of AKT and modulates receptor tyrosine kinase, RAF-MEK-MAPK and SRC/STAT signaling. Clin Cancer Res. 2012 Aug 1;18(15):4104-13.  

    Fimepinostat (CUDC-907)

    CUDC-907 suppresses tumor growth, inhibits HDAC activity, and blocks signaling of PI3K and MAPK pathways in xenograft models. Clin Cancer Res. 2012 Aug 1;18(15):4104-13. 


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