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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Endocrinology & Hormones > AilanthoneCAS：981-15-7
Molecular Formula：C20H24O7
Molecular Weight：376.4
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 981-15-7 |
| Name | Ailanthone |
| Molecular Formula | C20H24O7 |
| Molecular Weight | 376.4 |
| Solubility | Soluble in DMSO |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 683-145-8 |
| MDL | MFCD01729487 |
| SMILES | 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 |
| Target Point | Androgen Receptor |
| Passage | Endocrinology & Hormones |
| Background | Ailanthone is a potent androgen receptor (AR) inhibitor that inhibits the intact androgen receptor. |
| Biological Activity | Ailanthone是有效的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[1]。 |
| IC50 | 69 nM(Full-length androgen receptor)，309 nM(AR1-651)[1] |
| In Vitro | Ailanthone是全长AR(AR-FL)和组成型活性截短AR剪接变体(AR-Vs)的有效抑制剂。 Ailanthone与共伴侣蛋白p23结合并阻止AR与HSP90的相互作用，从而导致AR-伴侣复合物的破坏，随后泛素/蛋白酶体介导的AR降解以及其他p23客户包括AKT和Cdk4，以及下调AR及其在PCa细胞系和原位动物肿瘤中的靶基因。此外，Ailanthone阻断CRPC的肿瘤生长和转移[1]。已经显示，Ailanthone对几种癌细胞系具有生长抑制作用，包括HepG2，Hep3B，R-HepG2，Jurkat，HeLa，MCF-7，MDA-MB-231和A549细胞。 Ailanthone通过诱导线粒体介导的细胞凋亡和G0/G1细胞周期停滞来抑制Huh7细胞的生长。 Ailanthone诱导的细胞凋亡是线粒体介导的，并参与Huh7细胞中的PI3K/AKT信号通路[2]。 |
| In Vivo | 不仅ip给药而且对Ailanthone的口服给药具有阻止CRPC异种移植物生长的优异效率。在药代动力学研究中，Ailanthone在水中具有良好的溶解性和良好的生物利用度(> 20％)。此外，尽管在治疗过程中没有达到稳定的血浆药物浓度状态，但Ailanthone有效抑制了CRPC肿瘤的生长[1]。 |
| Cell Experiment | 对于SRB测定，将细胞在完全RPMI 1640中培养并与指定浓度的Ailanthone一起温育，或将细胞维持在含有5％活性炭剥离的FBS，1nM DHT和所示化合物的新鲜无酚红RPMI 1640培养基中。 48或72小时后，然后固定细胞并用SRB测定法检测细胞生长。对于集落形成测定，将前列腺癌细胞与指定浓度的Ailanthone在完全RPMI 1640中孵育2周，然后用4％多聚甲醛固定细胞并用结晶紫染色。在显微镜下观察菌落，并对所有田地进行成像和计数。提出了菌落形成作为每种细胞系的载体对照的百分比[1]。 |
| Animal Experiment | 小鼠[1]在原位去势抗性前列腺癌异种移植模型中，给小鼠腹膜内注射Ailanthone(2mg/kg)，MDV(10mg/kg)或DMSO(作为对照)。使用IVIS成像系统每周监测前列腺肿瘤生长和局部转移。使用Living Image和Xenogen软件[1]获取和分析生物发光信号的图像和测量值。 |
| Data Literature Source | [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 |
| Unit | Bottle |
| Specification | 5mg 10mM*1mL in DMSO 10mg |
是有效的雄激素受体 (androgen receptor (AR)) 抑制剂， 抑制完整雄激素受体。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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