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Ailanthone is a potent inhibitor of both full-length androgen receptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651 IC50=309 nM).
Ailanthone binds to the co-chaperone protein p23 and prevents AR's interaction with HSP90, thus resulting in the disruption of the AR-chaperone complex followed by ubiquitin/proteasome-mediated degradation of AR as well as other p23 clients including AKT and Cdk4, and downregulates AR and its target genes in PCa cell lines and orthotopic animal tumours. In addition, Ailanthone blocks tumour growth and metastasis of CRPC.
| Molecular Weight | 376.40 |
| Formula | C20H24O7 |
| CAS Number | 981-15-7 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] No authors listed. J Cell Biochem. Retraction
[2] Haixiang Ding, et al. Oncol Lett. Ailanthone: A novel potential drug for treating human cancer
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