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Ailanthone

Catalog No. TQ0209 CAS 981-15-7

Synonyms: Δ13-Dehydrochaparrinone

Ailanthone (Δ13-Dehydrochaparrinone) is an effective inhibitor of both full-length androgen receptor (AR) (IC50: 69 nM) and constitutively active truncated AR splice variants (IC50: 309 nM).

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Ailanthone, CAS 981-15-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
5 mg	In stock	$ 80.00
10 mg	In stock	$ 118.00
25 mg	In stock	Inquiry
50 mg	In stock	Inquiry
1 mL * 10 mM (in DMSO)	In stock	$ 89.00

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Purity: 99.78%

Purity: 99.71%

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Description	Ailanthone (Δ13-Dehydrochaparrinone) is an effective inhibitor of both full-length androgen receptor (AR) (IC50: 69 nM) and constitutively active truncated AR splice variants (IC50: 309 nM).
Targets&IC50	Androgen receptor:69 nM
In vitro	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 [1]. 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 [2].
In vivo	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 [1].
Cell Research	For SRB assay, cells are cultured in complete RPMI 1640 and incubated with indicated concentrations of Ailanthone or cells are maintained in fresh phenol red-free RPMI 1640 medium with 5% charcoal-stripped FBS, 1?nM DHT and indicated compounds. After 48 or 72?h, the cells are then fixed and the cell growth is detected with the SRB assay. For colony formation assay, prostate cancer cells are incubated with indicated concentrations of Ailanthone in complete RPMI 1640 for 2 weeks and then cells are fixed with 4% paraformaldehyde and stained with crystal violet. Colonies are visualized under a microscope, and all of the fields are imaged and counted. Colony formation as a percentage of vehicle control for each cell line is presented [1].
Animal Research	In the orthotopic castration-resistant prostate cancer xenografts model, mice are intraperitoneally injected with Ailanthone (2?mg/kg), MDV (10 mg/kg) or DMSO (as controls). Prostate tumor growth and local metastasis are monitored weekly using the IVIS Imaging System. Images and measurements of bioluminescent signals are acquired and analyzed using software [1].
Source	Natural Products > Simaroubaceae > Ailanthus

Synonyms	Δ13-Dehydrochaparrinone
Molecular Weight	376.4
Formula	C20H24O7
CAS No.	981-15-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (212.54 mM), Sonication is recommended.

References and Literature

1. He Y, et al. Ailanthone targets p23 to overcome MDV3100 resistance in castration-resistant prostate cancer. Nat Commun. 2016 Dec 13;7:13122. 2. Zhuo Z, et al. Ailanthone Inhibits Huh7 Cancer Cell Growth via Cell Cycle Arrest and Apoptosis In Vitro and In Vivo. Sci Rep. 2015 Nov 3;5:16185.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Covalent Inhibitor Library Selected Plant-Sourced Compound Library Covalent Natural Product Library Endocrinology-Hormone Compound Library Natural Product Library Anti-Cancer Compound Library Transcription Factor-Targeted Compound Library RO5 Drug-like Natural Product Library Anti-Tumor Natural Product Library

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Keywords

Ailanthone 981-15-7 Endocrinology/Hormones Androgen Receptor delta13-Dehydrochaparrinone inhibit Inhibitor Δ13-Dehydrochaparrinone inhibitor

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