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    Domatinostat (4SC202)
    Domatinostat (4SC202)

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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 #: V0264
    CAS #: 910462-43-0Purity ≥98%

    Description: Domatinostat (formerly 4SC-202) is a novel, potent, and orally bioavailable benzamide-based Class I HDAC inhibitor with potential anticancer activity. It inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 1.20 μM, 1.12 μM, and 0.57 μM, respectively. Domatinostat/4SC-202 acts by selectively binding to and inhibiting class I HDACs, which led to an accumulation of highly acetylated histones. 

    ReferencesTarget Oncol. 2016 Dec;11(6):783-798; 4sc-202-poster-eortc-berlin-2010 

    Related CAS #: 1186222-89-8 (tosylate)

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    Molecular Weight (MW)447.51
    FormulaC23H21N5O3S
    CAS No.910462-43-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO:89 mg/mL (198.9 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo) 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 10 mg/mL
    Synonyms4SC-202; 4SC202; 4SC 202; domatinostat


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    In Vitro

    In vitro activity: In HeLa cells, 4SC-202 induces hyperacetylation of histone H3 with EC50 of 1.1 μM. 4SC-202 induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM.


    Cell Assay: Domatinostat (4SC-202 free base) tosylate treatment induces potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. Domatinostat (4SC-202 free base) tosylate induces apoptosis signal-regulating kinase 1 (ASK1) activation, causing it translocation to mitochondria and physical association with Cyp-D

    In VivoOral gavage of Domatinostat (4SC-202 free base) inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened; In vivo, 4SC-202 has a high oral bioavailability, and shows high metabolic stability and a low plasma clearance. 4SC-202 (120 mg/kg p.o.) shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model.
    Animal modelNude mice
    Formulation & Dosage120 mg/kg p.o.
    References

    Zhijun H, et al. Pre-clinical characterization of 4SC-202, a novel class I HDAC inhibitor, against colorectal cancer cells. Tumour Biol. 2016 Aug;37(8):10257-67.; 4sc-202-poster-eortc-berlin-2010 


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

     

    4SC-202

    Impact of specific pharmacological inhibition of class I HDAC isoenzymes with 4SC-202 on UCCs and control cells. Target Oncol. 2016 Dec;11(6):783-798.
     

    4SC-202

    Mechanisms of cell death upon 4SC-202 treatment in UCCs and control cells. Target Oncol. 2016 Dec;11(6):783-798.
     

    4SC-202

    Aberrant nuclear morphology in 4SC-202 treated VM-CUB1 and UM-UC-3 cells. Target Oncol. 2016 Dec;11(6):783-798.


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