Journal: Cancer Research Communications

Article Title: Identification of an Imidazopyridine-based Compound as an Oral Selective Estrogen Receptor Degrader for Breast Cancer Therapy

doi: 10.1158/2767-9764.CRC-23-0111

Figure Lengend Snippet: X15695-mediated regulation of AR action in prostate cancer cells. A, Western blot analysis of BAG1 in LNCaP cells transduced with BAG-1 shRNA and control shRNA. Antibodies to vinculin, AR, tubulin, and GAPDH were used as controls. B, Quantification of the effect of X15695 on clonal expansion of control and BAG1 shRNA knockdown LNCaP cells. Each point represents the mean ± SEM. n = 3. C, Western blot analysis of AR and BAG1 in extracts of LNCaP and 22Rv.1 cells treated with the indicated concentrations of X15695 for 24 hours. β-actin was used as a loading control. D–F, GSEA plots of the topmost signaling pathways and heat maps of log 2 fold-change in gene expression in the comparison of DHT + X15695 versus DHT and X15695 versus vehicle in LNCaP cells. G, Quantitative RT-PCR was carried to detect the effect of X15695 on DHT- mediated expression of the indicated target genes in LNCaP cells. Cells were treated with vehicle or 10 nmol/L DHT and X15695 (5 μmol/L) for 16 hours. The results are the means ± SEM ( n = 4; *, P ≤ 0.05; ***, P ≤ 0.001; ****, P ≤ 0.0001; ns, not significant). H, 22Rv.1, LAPC-4, and LNCaP cells were transfected with control and p53 siRNA for 16 hours and treated with vehicle or X15695 (5 μmol/L) for 24 hours. Western blot analysis was performed with anti-p53 and anti-β-actin antibodies. I, MTT cell viability assay carried out with 22Rv.1, LAPC-4, and LNCaP cells previously transfected with control and p53 siRNA and treated with vehicle and X15695 for 72 hours. The results are the mean ± SEM ( n = 3; *, P ≤ 0.05).

Article Snippet: MCF-7 and LAPC-4 cells (2 × 10 6 ) were suspended in 100 μL PBS: Matrigel (Corning, 354248; 1:1) and injected subcutaneously into both flanks of 6–7 weeks old female (for MCF-7 cells) and male (for LAPC-4 cells) athymic nude- Foxn1 nu mice (Envigo 6901M).

Techniques: Western Blot, Transduction, shRNA, Expressing, Quantitative RT-PCR, Transfection, Viability Assay

Journal: Cancer Research Communications

Article Title: Identification of an Imidazopyridine-based Compound as an Oral Selective Estrogen Receptor Degrader for Breast Cancer Therapy

doi: 10.1158/2767-9764.CRC-23-0111

Figure Lengend Snippet: X15695 induces cell-cycle arrest and inhibits proliferation of AR + and ER + prostate and breast cancer cells. Cell-cycle profile measured by flow cytometry of LNCaP ( A ) and LAPC-4 cells ( B ) treated with vehicle or 1 μmol/L X15695 for 48 hours. Cells for flow cytometry were stained with DRAQ5. The quantified results are the mean ± SEM ( n = 3; *, P ≤ 0.05; **, P ≤ 0.01). C, Representative examples of LAPC-4 xenograft mouse tumors after daily treatment with vehicle, X15695 (10 and 30 mg/kg), and enzalutamide (10 mg/kg) for 43 days. D, Tumor weights at the end of treatment were recorded and presented as a bar chart. The values are the means ± SEM expressed (**, P ≤ 0.01; ****, P ≤ 0.0001; n = 14; ns, not significant). E, Mouse body weights were measured twice weekly over the 43 days. Presented are the mouse body weight changes, in percentages, for each group. F, Quantification of the effect of the indicated concentrations of X15695 on clonal expansion of the indicated tumor cells ( n = 3).

Article Snippet: MCF-7 and LAPC-4 cells (2 × 10 6 ) were suspended in 100 μL PBS: Matrigel (Corning, 354248; 1:1) and injected subcutaneously into both flanks of 6–7 weeks old female (for MCF-7 cells) and male (for LAPC-4 cells) athymic nude- Foxn1 nu mice (Envigo 6901M).

Techniques: Flow Cytometry, Staining

Journal: American Journal of Cancer Research

Article Title: Immuno-PET imaging of VEGFR-2 expression in prostate cancer with 89 Zr-labeled ramucirumab

doi:

Figure Lengend Snippet: The VEGFR-2 expression in prostate cancer (PrCa) cell lines measured by flow cytometry. The percentage of cell counts are from the same gate of top positive cells in fluorescent intensity in the three PrCa cell lines. Sample groups: Anti-r 2nd Ab only, the controls engaging with Alexa488 anti-rabbit secondary antibody only; Anti-h 2nd Ab only, the controls engaging with Alexa488 anti-human secondary antibody only; 55B11 as 1st Ab, the samples engaging with rabbit anti-human 55B11 as the primary antibody; Df-R as 1st Ab, the samples engaging with deferoxamine-conjugated Ramucirumab as the primary antibody (for PC-3 cell line, n = 4; for LAPC-4 and LNCAP cell lines, n = 3).

Article Snippet: X.0.7; Tree Star, Inc.; Ashland, OR), shift values of the top 1% of the positive counts in fluorescent intensity were gated on the histograms of LAPC-4 blank cells as the baseline control.

Techniques: Expressing, Flow Cytometry

Journal: American Journal of Cancer Research

Article Title: Immuno-PET imaging of VEGFR-2 expression in prostate cancer with 89 Zr-labeled ramucirumab

doi:

Figure Lengend Snippet: The uptake kinetics of the region of interest (ROI) in the positron emission tomography (PET) images of the three prostate cancer (PrCa) models (for the models bearing PC-3 tumors without/with pre-blockade, n = 3; for the models bearing LAPC-4 and LNCAP tumors, n = 4). P < 0.05.

Article Snippet: X.0.7; Tree Star, Inc.; Ashland, OR), shift values of the top 1% of the positive counts in fluorescent intensity were gated on the histograms of LAPC-4 blank cells as the baseline control.

Techniques: Positron Emission Tomography

Journal: American Journal of Cancer Research

Article Title: Immuno-PET imaging of VEGFR-2 expression in prostate cancer with 89 Zr-labeled ramucirumab

doi:

Figure Lengend Snippet: The typical positron emission tomography (PET) maximum-intensity projections (MIP) of the PC-3 (unblocked/pre-blocked), LNCAP and LAPC-4 prostate cancer (PrCa) models. Arrows point to the xenograft tumor of each group at 96 h p.i.

Article Snippet: X.0.7; Tree Star, Inc.; Ashland, OR), shift values of the top 1% of the positive counts in fluorescent intensity were gated on the histograms of LAPC-4 blank cells as the baseline control.

Techniques: Positron Emission Tomography

Journal: American Journal of Cancer Research

Article Title: Immuno-PET imaging of VEGFR-2 expression in prostate cancer with 89 Zr-labeled ramucirumab

doi:

Figure Lengend Snippet: The radioactive ex-vivo bio-distribution in the tumors and major organs of the three prostate cancer (PrCa) models (for the models bearing PC-3 tumors without/with blockade, n = 3; for the models bearing LAPC-4 and LNCAP tumors, n = 4). P < 0.05.

Article Snippet: X.0.7; Tree Star, Inc.; Ashland, OR), shift values of the top 1% of the positive counts in fluorescent intensity were gated on the histograms of LAPC-4 blank cells as the baseline control.

Techniques: Ex Vivo