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Ailanthone (Synonyms: Δ13-Dehydrochaparrinone)

Cat. No.: HY-N1943 Purity: 99.71%
Handling Instructions

Ailanthone (Δ13-Dehydrochaparrinone) 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).

For research use only. We do not sell to patients.

Ailanthone Chemical Structure

Ailanthone Chemical Structure

CAS No. : 981-15-7

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10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
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Description

Ailanthone (Δ13-Dehydrochaparrinone) 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).

IC50 & Target

IC50: 69 nM (Full-length androgen receptor), 309 nM (AR1-651)[1]

In Vitro

Ailanthone is a potent inhibitor of both full-length AR (AR-FL) and constitutively active truncated AR splice variants (AR-Vs). 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[1]. Ailanthone has been shown to possess an growth-inhibitory effect against several cancer cell lines including HepG2, Hep3B, R-HepG2, Jurkat, HeLa, 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

Not only i.p. administration but also p.o. administration of Ailanthone 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 tumour growth, despite not reaching a steady state of plasma drug concentration during the course of treatment[1].

Molecular Weight

376.40

Formula

C₂₀H₂₄O₇

CAS No.

981-15-7

SMILES
Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.3 mg/mL (221.31 mM; Need warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6567 mL 13.2837 mL 26.5675 mL
5 mM 0.5313 mL 2.6567 mL 5.3135 mL
10 mM 0.2657 mL 1.3284 mL 2.6567 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]

In 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 tumour growth and local metastasis are monitored weekly using the IVIS Imaging System. Images and measurements of bioluminescent signals are acquired and analysed using Living Image and Xenogen software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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