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    Tacedinaline (GOE-5549, PD-123654, CI-994; Acetyldinaline)
    Tacedinaline (GOE-5549, PD-123654, CI-994; Acetyldinaline)

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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 #: V0292
    CAS #: 112522-64-2Purity ≥98%

    Description: Tacedinaline (GOE5549, PD123654, CI994; Acetyldinaline) is a potent, orally bioavailable and selective inhibitor of histone deacetylase 1/3 (HDAC1/3) with potential anticancer activity. It inhibits HDAC1/2/3 with IC50s of 0.9, 0.9, 1.2 μM, respectively.

    References: J Med Chem. 2007;50(23):5543-6; Bioorg Med Chem. 2008;16(6):3352-60; Invest New Drugs. 1996;14(4):349-56. 

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    Molecular Weight (MW)269.3
    CAS No.112522-64-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 54 mg/mL (200.5 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
    SynonymsPD-123654, GOE-5549, Acetyldinaline, Tacedinaline; CI994, CI-994, CI 994, PD123654, PD-123654, PD 123654; N-acetyldinaline; Goe5549;  Goe 5549

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    In Vitro

    In vitro activity: CI-994 (< 160 mM) shows cytostatic effect with concomitant increase at G0/G1 phase, a reduction at S phase level and increased apoptosis in A-549 and LX-1 cells. CI-994 inhibits growth of LNCaP cell with IC50 of 7.4 μM. CI-994 exerts activity against several tumor cell lines with greater cytotoxicity against the solid tumors relative to both the leukemia and normal fibroblast cell lines. CI-994 inhibits growth of rat leukemia BCLO cells with IC50 of 2.5 μM.

    Kinase Assay: Tacedinaline (N-acetyldinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively.

    Cell Assay: LNCaP cell lines are maintained in RPMI 1640 medium containing 10% fetal bovine serum, 1% penicillin and streptomycin, as the complete culture medium. Cells (2×104) are seeded in 24-well plates and incubated in a 5% CO2 incubator at 37 °C for 1 day. Cultures are treated with CI-994, alone and in combination on day 2 and 4. Cells are washed on day 2 and 4 and media are changed. Mitochondrial metabolism is measured as a marker for cell growth by adding 100 μL/well MTT (5 mg/mL in medium) with 2 hours incubation at 37 °C on Day 6. Crystals formed are dissolved in 500 μL of DMSO. The absorbance is determined using a microplate reader at 560 nm. The absorbance data are converted into cell proliferation percentage. Each assay is performed in triplicate.

    In VivoCI-994 exerts demonstrated antitumor activity against several tumor models, including the chemo-resistant mouse pancreatic ductal carcinoma as well as the human prostate tumor model LNCaP.
    Animal modelHuman prostate tumor model LNCaP
    Formulation & DosageDissolved in 5% ethanol, 1% P.O.E. and 94% dH20; Oral gavage
    ReferencesJ Med Chem. 2007 Nov 15;50(23):5543-6; Oncol Res. 2005;15(1):39-48; Bioorg Med Chem. 2008 Mar 15;16(6):3352-60; Invest New Drugs. 1996;14(4):349-56. 

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


    CI994 (Tacedinaline)

    CI994 (Tacedinaline)
    The effect of various HDACIs in combination with retinoids or RAMBAs on LNCaP cell viability as assessed by the MTT assay. Bioorg Med Chem. 2008 Mar 15;16(6):3352-60. 
    CI994 (Tacedinaline)
    Western blot analysis for various proteins in LNCaP whole cell lysates after a 24 hour treatment with VN/66-1 (1.0 µM), SAHA (10 nM) or their combination. Bioorg Med Chem. 2008 Mar 15;16(6):3352-60. 


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