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ASC-J9

Cat. No. M8908
ASC-J9 Structure
Synonym:

GO-Y025; Dimethylcurcumin

Size Price Availability Quantity
20mg USD 500  USD500 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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. 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.

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. 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. ASC-J9-treated mice show significantly smaller prostate tumor sizes when compared with those receiving classic ADT/castration with little serum androgen.

Protocol
Cell Experiment
Cell lines PC12/AR-112Q and PC12/AR-10Q cells
Preparation method 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.
Concentrations
Incubation time
Animal Experiment
Animal models both anterior prostates of castrated nude mouse
Formulation
Dosages 75 mg/kg
Administration intraperitoneal injection
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 396.43
Formula C23H24O6
CAS Number 52328-98-0
Purity >98%
Solubility DMSO
Storage at -20°C
References

[1] Ma W, et al. Biochem Biophys Res Commun. Targeting androgen receptor with ASC-J9 attenuates cardiac injury and dysfunction in experimental autoimmune myocarditis by reducing M1-like macrophage.

[2] Yamashita S, et al. Neoplasia. ASC-J9 suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.

[3] Yang Z, et al. Nat Med. ASC-J9 ameliorates spinal and bulbar muscular atrophy phenotype via degradation of androgen receptor.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ASC-J9, GO-Y025; Dimethylcurcumin supplier, Androgen Receptor, inhibitors

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