臭椿酮 TQ0209

Product Introduction
Bioactivity


英文名: Ailanthone

描述: Ailanthone (Δ13-Dehydrochaparrinone) 是一种有效的雄激素受体 (androgen receptor (AR)) 抑制剂，能够抑制完整雄激素受体(IC50:69 nM)、持续活跃剪切变体(IC50:309 nM)。

细胞实验: 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].

动物实验: 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].

体外活性: Ailanthone通过结合共伴侣蛋白p23，阻止AR与HSP90的相互作用，从而破坏AR-伴侣复合体，进而通过泛素/蛋白酶体介导的途径促进AR以及包括AKT和Cdk4在内的其他p23客户蛋白的降解，下调PCa细胞系和原位动物肿瘤中AR及其靶基因的表达。此外，Ailanthone能够阻断CRPC的肿瘤生长和转移[1]。Ailanthone对包括R-HepG2、Jurkat、HeLa、HepG2、Hep3B、MCF-7、MDA-MB-231及A549细胞在内的多个癌细胞系显示出生长抑制作用。Ailanthone通过诱导线粒体介导的细胞凋亡和G0/G1细胞周期停滞，抑制Huh7细胞生长。Ailanthone诱导的凋亡是线粒体介导的，并在Huh7细胞中涉及PI3K/AKT信号通路[2]。

体内活性: Ailanthone（i.p.或p.o.）在阻断CRPC异种移植瘤生长方面展现出卓越的效能。药动学研究表明，Ailanthone在水中具有良好的溶解度和良好的生物利用度（>20%）。此外，尽管在治疗过程中未达到血浆药物浓度的稳态，Ailanthone仍有效地抑制CRPC肿瘤生长[1]。

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

溶解度: DMSO : 80 mg/mL (212.54 mM)


关键字: delta13-Dehydrochaparrinone | Ailanthone | inhibit | Inhibitor | Androgen Receptor

相关产品: SK33 | 2-hydroxy Flutamide | GSK-2881078 | RU 59063 | Bifluranol | Nandrolone phenylpropionate | AZD3514 | Nilutamide | Metenolone acetate | BMS-641988

相关库: 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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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途