Ailanthone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ailanthone (Δ13-Dehydrochaparrinone) 是有效的雄激素受体 (androgen receptor (AR)) 抑制剂， 抑制完整雄激素受体，和持续活跃剪切变体的 IC50 值分别为 69 nM 和309 nM。

Ailanthone is an effective inhibitor of both full-length androgen receptor (AR) (IC50: 69?nM) and constitutively active truncated AR splice variants (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 tumors. In addition, Ailanthone blocks tumor growth and metastasis of CRPC. Ailanthone has been shown to possess a growth-inhibitory effect against several cancer cell lines including R-HepG2, Jurkat, HeLa, HepG2, Hep3B, MCF-7, MDA-MB-231, and A549 cells. Ailanthone inhibits Huh7 cell growth through the induction of mitochondrion-mediated cell apoptosis and G0/G1 cell cycle arrest. Ailanthone-induced apoptosis is mitochondrion-mediated and involved the PI3K/AKT signaling pathway in Huh7 cells.Ailanthone (i.p. or p.o.) has excellent efficiency for blocking the growth of CRPC xenografts. In pharmacokinetic studies, Ailanthone exhibits good solubility in water and good bioavailability (>20%). In addition, Ailanthone effectively suppresses CRPC tumor growth, despite not reaching a steady state of plasma drug concentration during the course of treatment.

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Δ13-Dehydrochaparrinone

Endocrinology/Hormones

Androgen Receptor (AR)

Androgen Receptor

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981-15-7

376.4

C20H24O7

>98% (HPLC)

DMSO:80 mg/mL (212.54 mM; Need warming)

C[C@@]1([C@@H]2O)[C@]([C@@]3([C@@H]4O)O)([H])[C@@]([C@](C5)([H])C4=C)(CO3)[C@@](OC5=O)([H])C[C@@]1([H])C(C)=CC2=O

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(-20℃)

With Ice Pack

≥ 2 years