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    HJC0152 hydrochloride
    HJC0152 hydrochloride

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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 #: V2741
    CAS #: 1420290-99-8Purity ≥98%

    Description: HJC0152 hydrochloride is a novel, orally bioavailable and potent inhibitor of the signal transducers and activators of transcription 3 (STAT3). It has potential application for treating human head and neck squamous cell carcinoma (HNSCC). HJC0152 has been demonstrated to significantly suppress MDA-MB-231 xenograft tumor growth in vivo (i.p. & p.o.), indicating its great potential as efficacious and orally bioavailable therapeutics for human cancers. HJC0152 was designed and developed based on niclosamide which has been identified to potently inhibit the activation, nuclear translocation, and transactivation of STAT3 but with pharmacokinetics such as poor aqueous solubility and bioavailability of niclosamide. HJC0152 has improved pharmacokinetic profiles.

    References:  2013 Feb 14;4(2):180-185. 


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    Molecular Weight (MW) 406.64
    Formula C15H14Cl3N3O4 
    CAS No. 1420290-99-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 5 mg/mL (under ultrasonic condition)
    Water: N/A
    Ethanol: N/A
    Chemical Name 2-(2-Amino-ethoxy)-5-chloro-N-(2-chloro-4-nitrophenyl)benzamide Hydrochloride
    Synonyms HJC0152; HJC 0152 HCl; HJC-0152 hydrochloric acid
    SMILES Code O=C(NC1=CC=C([N+]([O-])=O)C=C1Cl)C2=CC(Cl)=CC=C2OCCN.[H]Cl


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    In Vitro

    In vitro activity: compound 11 (HJC0152 hydrochloride) significantly inhibits cell proliferation and induces apoptosis accompanying cellular morphological changes at concentrations of 1, 5, and 10 μM. Results show that treatment with 10 μM HJC0152 hydrochloride decreases the STAT3 promoter activity in MDA-MB-231 cells by approximately 32%, and increasing the dose of HJC0152 hydrochloride to 20 μM further decreases STAT3 promoter activity by 62% as compare with control. Total STAT3 is reduced after treatment with HJC0152 hydrochloride. HJC0152 hydrochloride induces cleaved caspase-3 and down regulates cyclin D1 in MDA-MB-231 cells. 


    Kinase Assay: HJC0152 hydrochloride is a novel, orally bioavailable and potent inhibitor of the signal transducers and activators of transcription 3 (STAT3). It has potential application for treating human head and neck squamous cell carcinoma (HNSCC). 


    Cell Assay: Breast cancer MDA-MB-231 cells are incubated in 6-well plates (2.5×105/well). Cells are then treated with DMSO, or HJC0152 hydrochloride (compound 11) at different concentrations for 48 h, and then both adherent and floating cells are collected, washed once with PBS. Resuspended cells are incubated with 100 μL PBS containing 1% BSA and 100 μL Annexin V and dead cell detection reagent at room temperature for 20 min. Apoptosis is measured immediately using the Muse Cell Analyzer with the MuseTM Apoptosis Kit. 

    In VivoMice treated with 7.5 mg/kg of HJC0152 hydrochloride (compound 11) via ip show a better effect in inhibiting tumor growth. The growth of xenograft tumors in mice is significantly reduced by HJC0152 hydrochloride at a dose of 25 mg/kg. It is also noteworthy that HJC0152 hydrochloride does not show significant signs of toxicity at a dose of 75 mg/kg. Fifty-four female nude mice are are used for orthotopic tumor studies at 4 to 6 weeks of age. The mice are maintained in a barrier unit with 12 h light-dark switch. Freshly harvested MDA-MB-231 cells (2.5×106 cells per mouse, resuspended in 100 μL PBS) are injected into the 3rd mammary fat pad of the mice, and then randomly assigned into 8 groups (5 to10 mice per group). For the intraperitoneal treatment experiment, the mice are treated daily with 2.5 mg/kg HJC0152 hydrochloride (compound 11) (Group A) or vehicle (Group D) when the tumor volume reaches 200 mm3. A Body weights and tumors volume are measured daily and tumor volume is calculated according to the formula V=0.5×L×W2, where L=length (mm) and W=width (mm)
    Animal model Female nude mice
    Formulation & Dosage 7.5 mg/kg; i.p.
    References  2013 Feb 14;4(2):180-185.


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

    HJC0152 hydrochloride

    In vivo efficacy of compound 11 (HJC0152) in inhibiting growth of xenograft tumors (breast cancer MDA-MB-231) in mice. (A) ip and (B) po.  2013 Feb 14;4(2):180-185.

     

    HJC0152 hydrochloride

    (A) HJC0152 inhibited the STAT3-mediated luciferase reporter activity in MDA-MB-231 cells. (B) Proliferation of MDA-MB-231 cells treated with HJC0152 and niclosamide for 24 h. 2013 Feb 14;4(2):180-185.

     

    HJC0152 hydrochloride

    (A) Western blot analysis of biochemical markers for apoptosis induction and inhibition of STAT3 activity by HJC0152 in the MDA-MB-231 cell line. (B) Densitometric analysis of three independent experiments for the expression level of total STAT3, phospho-STAT3, cyclin D1, and cleaved caspase 3.  2013 Feb 14;4(2):180-185.


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