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ASC-J9

Catalog No.
A3190
AR degradation enhancer,antiumor agent
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$72.00
In stock
5mg
$66.00
In stock
10mg
$110.00
In stock
50mg
$396.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

ASC-J9 (CAS 52328-98-0) is a small-molecule degrader targeting androgen receptor (AR). By promoting degradation of full-length AR and splice variants such as AR3/fAR, ASC-J9 inhibits androgen receptor signaling pathways involved in castration-resistant prostate cancer (CRPC) progression and metastatic behavior. ASC-J9 interferes with AR-dependent transcriptional modulation and AR-independent signaling pathways, notably inhibiting STAT3 phosphorylation and CCL2 chemokine secretion, thus reducing macrophage infiltration and prostate cancer invasiveness. Research indicates ASC-J9 may represent an alternative therapeutic strategy for CRPC treatment and metastasis prevention.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt396.43
Cas No.52328-98-0
FormulaC23H24O6
SynonymsGO-Y025; Dimethylcurcumin; ASC J9; GO Y025
Solubilityinsoluble in EtOH; insoluble in H2O; ≥16.65 mg/mL in DMSO
Chemical Name(1E,4Z,6E)-1,7-bis(3,4-dimethoxyphenyl)-5-hydroxyhepta-1,4,6-trien-3-one
SDFDownload SDF
Canonical SMILESCOC1=CC(/C=C/C(/C=C(O)/C=C/C2=CC=C(OC)C(OC)=C2)=O)=CC=C1OC
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

Human C4-2B/human THP1 cells and mouse TRAMP-C1/mouse RAW264.7 cells.

Preparation method

Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

5 μM; 3 days.

Applications

ASC-J9 suppresses macrophage recruitment and suppresses PCa invasion.

Animal experiment [1]:

Animal models

Male 6- to 8-week-old nude mice with orthotopically xenografted 106 TRAMP-C1 cells.

Dosage form

75 mg/kg; i.p. injected three times per week for 3 weeks.

Applications

In mice, ASC-J9 significantly decreases developing distant metastatic tumors in diaphragm and lymph nodes. There are little change in mice body weight among all the mice treated.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Lin TH, Izumi K, Lee SO, et al. Anti-androgen receptor ASC-J9 versus anti-androgens MDV3100 (Enzalutamide) or Casodex (Bicalutamide) leads to opposite effects on prostate cancer metastasis via differential modulation of macrophage infiltration and STAT3-CCL2 signaling. Cell Death Dis, 2013, 4: e764.

Biological Activity

Description ASC-J9 is an enhancer of androgen receptor degradation.
Targets PC-3 cell proliferation LNCaP cell proliferation        
IC50 5.9 μM 3.9 μM        

Quality Control