Product Introduction
Bioactivity


英文名: Ailanthone

描述: Ailanthone (Δ13-Dehydrochaparrinone) 是一種有效的雄激素受體 (androgen receptor (AR)) 抑制劑，能夠抑制完整雄激素受體(IC50:69 nM)、持續(xù)活躍剪切變體(IC50:309 nM)。

細胞實驗: 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].

動物實驗: 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].

體外活性: Ailanthone通過結(jié)合共伴侶蛋白p23，阻止AR與HSP90的相互作用，從而破壞AR-伴侶復合體，進而通過泛素/蛋白酶體介導的途徑促進AR以及包括AKT和Cdk4在內(nèi)的其他p23客戶蛋白的降解，下調(diào)PCa細胞系和原位動物腫瘤中AR及其靶基因的表達。此外，Ailanthone能夠阻斷CRPC的腫瘤生長和轉(zhuǎn)移[1]。Ailanthone對包括R-HepG2、Jurkat、HeLa、HepG2、Hep3B、MCF-7、MDA-MB-231及A549細胞在內(nèi)的多個癌細胞系顯示出生長抑制作用。Ailanthone通過誘導線粒體介導的細胞凋亡和G0/G1細胞周期停滯，抑制Huh7細胞生長。Ailanthone誘導的凋亡是線粒體介導的，并在Huh7細胞中涉及PI3K/AKT信號通路[2]。

體內(nèi)活性: Ailanthone（i.p.或p.o.）在阻斷CRPC異種移植瘤生長方面展現(xiàn)出卓越的效能。藥動學研究表明，Ailanthone在水中具有良好的溶解度和良好的生物利用度（>20%）。此外，盡管在治療過程中未達到血漿藥物濃度的穩(wěn)態(tài)，Ailanthone仍有效地抑制CRPC腫瘤生長[1]。

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

溶解度: DMSO : 80 mg/mL (212.54 mM)


關(guān)鍵字: delta13-Dehydrochaparrinone | Ailanthone | inhibit | Inhibitor | Androgen Receptor

相關(guān)產(chǎn)品: SK33 | 2-hydroxy Flutamide | GSK-2881078 | RU 59063 | Bifluranol | Nandrolone phenylpropionate | AZD3514 | Nilutamide | Metenolone acetate | BMS-641988

相關(guān)庫: Anti-Prostate Cancer Compound Library | Selected Plant-Sourced Compound Library | Covalent Natural Product Library | Inhibitor Library | Nuclear Receptor Compound Library | Traditional Chinese Medicine Monomer Library | Natural Product Library for HTS | RO5 Drug-like Natural Product Library | Covalent Inhibitor Library | NO PAINS Compound Library

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