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    Galeterone
    Galeterone

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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 #: V0811
    CAS #: 851983-85-2Purity ≥98%

    Description: Galeterone (formerly known as NX 41765; TOK001; VN/124-1; NX-41765; VN-1241; TOK-001) is a novel, potent and selective, orally bioavailable CYP17 lyase inhibitor and androgen receptor (AR) antagonist with potential anticancer activity. It inhibits CYP17 and AR with IC50s of 300 nM and 384 nM, respectively. 

    References: J Med Chem. 2005 Apr 21;48(8):2972-84; Mol Cancer Ther. 2008 Aug;7(8):2348-57.

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    Molecular Weight (MW)388.55
    FormulaC26H32N2O
    CAS No.851983-85-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 24 mg/mL (61.8 mM) 
    Water: <1 mg/mL
    Ethanol: 40 mg/mL (102.9 mM)
    Solubility (In vivo)0.5% hydroxyethyl cellulose: 30 mg/mL  
    SynonymsGaleterone; NX41765; NX 41765; TOK001; NX-41765; VN 1241; TOK-001; TOK 001; VN-1241; VN-1241 

    Chemical Name: (3S,8R,9S,10R,13S,14S)-17-(1H-benzo[d]imidazol-1-yl)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol

    InChi Key: PAFKTGFSEFKSQG-PAASFTFBSA-N

    InChi Code: InChI=1S/C26H32N2O/c1-25-13-11-18(29)15-17(25)7-8-19-20-9-10-24(26(20,2)14-12-21(19)25)28-16-27-22-5-3-4-6-23(22)28/h3-7,10,16,18-21,29H,8-9,11-15H2,1-2H3/t18-,19-,20-,21-,25-,26-/m0/s1

    SMILES Code: O[[email protected]]1CC[[email protected]]2(C)[[email protected]@]3([H])CC[[email protected]]4(C)C(N5C=NC6=CC=CC=C56)=CC[[email protected]@]4([H])[[email protected]]3([H])CC=C2C1           


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    In Vitro

    In vitro activity: Galeterone is effective at preventing binding of [3H]-R1881 to the mutant LNCaP AR (T877A) with IC50 of 845 nM. Galeterone inhibits the DHT-induced proliferation of LNCaP and LAPC4 cells in a dose-dependent manner with IC50 of 6 μM and 3.2 μM, respectively. Galeterone also inhibits the binding of [3H]-R1881 to the T575A mutant AR in PC3 cells with IC50 of 454 nM. Galeterone potently inhibits the proliferation of LNCaP and LAPC4 cells in the absence of DHT stimulation with IC50 of 2.6 μM and 4 μM, respectively. Furthermore, Galeterone treatment increases the degradation rate of the AR in a dose-dependent manner. Galeterone potently inhibits the growth of the androgen-independent cell lines PC-3 and DU-145 in a dose-dependent manner with GI50 of 7.82 μM and 7.55 μM, respectively. Galeterone induces the endoplasmic reticulum stress response resulting in down-regulation of cyclin D1 protein expression and cyclin E2 mRNA. Galeterone effectively inhibits proliferation of HP-LNCaP and C4-2B cell lines with IC50 of 2.9 μM and 9.7 μM, respectively. Galeterone treatment at 1 μM effectively inhibits androgen receptor activation in LNCaP cells (50%) and HP-LNCaP cells (70%). Galeterone decreases activation of the androgen receptor in both LNCaP cells and HP-LNCaP cells with IC50 of 1 μM and 411 nM, respectively, and down-regulates androgen receptor protein expression by 50% after 24 hour of treatment. Galeterone reduces AR protein and mRNA expression, antagonizes AR-dependent promoter activation induced by androgen, and significantly reduces the phospho-4EBP1 levels.


    Kinase Assay: The in vitro CYP17 inhibitory activity of Galeterone is evaluated using rapid acetic acid releasing assay (AARA), utilizing intact P450c17-expressing E. coli as the enzyme source. It involves the use of [21-3H]-17α-hydroxypregnenolone as the substrate, and CYP17 activity is measured by the amount of tritiated acetic acid formed during the cleavage of the C-21 side chain of the substrate. IC50 value is obtained directly from plots relating percentage inhibition versus inhibitor concentration over appropriate ranges. 


    Cell Assay: Cells (LNCaP and LAPC4) are seeded in 24 well multi-well plates. Cells are treated with the increasing concentration of Galeterone in steroid free medium with or without 1 nM DHT (LNCaP), or 10 nM DHT (LAPC4) and allowed to grow for 7 days. The number of viable cells is compared by MTT assay (LAPC4) or XTT assay (LNCaP) on the 7th day.

    In VivoAdministration of Galeterone at 50 mg/kg twice daily is very effective at inhibiting the growth of androgen-dependent LAPC4 human prostate tumor xenograft, with a 93.8% reduction in the mean final tumor volume compared with controls, and it is also significantly more effective than castration. Treatment of Galeterone (0.13 mM/kg twice daily) or Galeterone (0.13 mmol/kg twice daily) plus castration induces regression of LAPC4 tumor xenografts in SCID mice by 26.55% and 60.67%, respectively. Treatments with Galeterone or Galeterone plus castration causes marked reduction in AR protein of 10- and 5-fold, respectively. 
    Animal modelMale severe combined immunodeficient (SCID) mice inoculated subcutaneously (s.c.) with LAPC4 cells 
    Formulation & DosageDissolved in a 0.3% solution of hydroxypropyl cellulose in saline; 50 mg/kg; s.c. injection
    References

    J Med Chem. 2005 Apr 21;48(8):2972-84; Mol Cancer Ther. 2008 Aug;7(8):2348-57.


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

    Galeterone


    Western Blot Analysis of AR expression in vitro (VN/124-1 is Galeterone). Mol Cancer Ther. 2008 Aug;7(8):2348-57.
     

    Galeterone

    Effect of compounds on DHT stimulated transcription. Mol Cancer Ther. 2008;7(8):2348-57.



    Galeterone


    Effects of VN/124-1, casodex, and castration on the prevention and growth of LAPC4 human prostate xenografts in male SCID mice.
     

    Galeterone


    Western immunobloting analysis of whole cell lysates from LAPC4 tumors following various treatments.



    Galeterone

    Percent change in mouse body weight over treatment duration in LAPC4 human prostate cancer xenografts in male SCID mice. Mol Cancer Ther. 2008 Aug;7(8):2348-57.


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