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CT-189

Chemical Structure : CT-189

CAS No.: 1541941-57-4

CT-189 (CT189)

Catalog No.: PC-49215Not For Human Use, Lab Use Only.

CT-189 (CT189) is a drug-like analog of IPAG and small-molecule Sigma1 receptor inhibitor, binds Sigma1 with Ki value of 38 nM in [3H](+)-pentazocine binding competition assays.

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    Biological Activity

    CT-189 (CT189) is a drug-like analog of IPAG and small-molecule Sigma1 receptor inhibitor, binds Sigma1 with Ki value of 38 nM in [3H](+)-pentazocine binding competition assays.
    CT-189 inhibits androgen receptor (AR) transcriptional activity and AR splice variant (ARV) signaling, decreases KLK3/PSA mRNA transcript levels in LNCaP cells and 22Rv1 cells, decreases levels of ARV7 as well as AR protein levels.
    CT-189 prevents 5α-dihydrotestosterone (DHT)-mediated nuclear translocation of AR and induced proteasomal degradation of AR and ARV, suppressing the transcriptional activity and protein levels of both full-length and splice-variant AR.
    CT-189 (30 mg/kg, oral gavage) inhibits the growth of xenografted 22Rv1 tumors by 60% following -36 days of treatment.

    Physicochemical Properties

    M.Wt 321.780
    Formula C16H17ClFN3O
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    1-(4-chlorophenyl)-3-(3-(4-fluorophenoxy)propyl)guanidine

    References

    1. Jeffrey D. Thomas, et al. Cancer Res. 2017 May 1; 77(9): 2439–2452.

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