Description |
ASC-J9 is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
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In Vitro |
ASC-J9 is able to degrade fAR and AR3 in a dose-dependent manner in various human PCa cells. ASC-J9 can also effectively suppress AR-targeted genes in CWR22Rv1-fARKD cells. ASC-J9 (5 or 10 µM) significantly suppresses the DHT-induced cell growth in all three PCa cell lines. ASC-J9 suppresses AR-targeted genes and cell growth by degradation of fAR and ectopic AR3 in C81 and C4-2 cells[1]. ASC-J9 selectively promotes AR degradation by disrupting the interaction between AR and AR coregulators. ASC-J9 reduces the AR aggregated AR-112Q in cells. ASC-J9 suppresses the aggregation of AR-112Q in SBMA PC12/AR-112Q cells[2].
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In Vivo |
ASC-J9 (75 mg/kg, i.p.) degrades both fAR and AR3 in the xenografted tumors in vivo, and SC-J9-treated tumors has significantly decreased Ki67-positive cells[1]. ASC-J9 (50 mg/kg every 48 h, i.p.) substantially ameliorates the SBMA symptoms in AR-97Q mice, and ameliorates neuromuscular pathological findings. The ASC-J9-treated SBMA mice have relatively normal serum testosterone concentrations[2]. ASC-J9-treated mice show significantly smaller prostate tumor sizes when compared with those receiving classic ADT/castration with little serum androgen[3].
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Cell Assay |
For the cell survival assay, the PC12/AR-112Q and PC12/AR-10Q cells are cultured as described previously and incubated cells in the presence of 10 μg/mL doxycycline for 24 h. Then the cells are treated with vehicle, 5 μM ASC-J9 or 10 μM ASC-J9, along with 1 nM DHT, and determined cell viability using Trypan blue staining at specific time intervals.
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Animal Admin |
CWR22Rv1 cells (1×106 cells per site) are injected into both anterior prostates of castrated nude mouse after 2 weeks of implantation. The mice are randomLy divided into two groups (four mice/eight tumors each group) and either receives 75 mg/kg ASC-J9 intraperitoneal injection or vehicle control every other day. After 4 weeks of treatment, all mice are killed to examine the tumor growth. Body weights and mice activity are measured weekly.
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Density | 1.2±0.1 g/cm3 |
Boiling Point | 588.6±50.0 °C at 760 mmHg |
Flash Point | 201.8±23.6 °C |
Exact Mass | 396.157288 |
PSA | 74.22000 |
LogP | 4.05 |
Vapour Pressure | 0.0±1.7 mmHg at 25°C |