Ailanthone (δ13-Dehydrochaparrinone)
(Synonyms: 臭椿酮,Δ13-Dehydrochaparrinone) 目录号 : GC31742
A quassinoid with diverse biological activities
Cas No.:981-15-7
Sample solution is provided at 25 µL, 10mM.
Ailanthone is a quassinoid that has been found in Ailanthus and has diverse biological activities.1,2,3 It is active against the P. falciparum strains HB-3 and Dd-2 in vitro (IC50s = 0.003 and 0.037 μg/ml, respectively).1 Ailanthone is phytotoxic, inhibiting radish seed germination by 88% when used at a concentration of 1 mM.2 It inhibits dihydrotestosterone-induced androgen receptor transcriptional activity (IC50 = 69 nM in a reporter assay), as well as the growth and colony formation of LNCaP and 22RV1 androgen receptor-expressing cells, but not androgen receptor-negative PC3 and DU145 cells, when used at a concentration of 0.1 μM.3 Ailanthone (2 mg/kg) reduces tumor volume in 22Rv1, LNCaP, and VCaP castration-resistant prostate cancer (CRPC) mouse xenograft models.
1.Okunade, A.L., Bikoff, R.E., Casper, S.J., et al.Antiplasmodial activity of extracts and quassinoids isolated from seedlings of Ailanthus altissima (Simaroubaceae)Phytother. Res.17(6)675-677(2003) 2.De Feo, V., De Martino, L., Quaranta, E., et al.Isolation of phytotoxic compounds from tree-of-heaven (Ailanthus altissima swingle)J. Agric. Food Chem.51(5)1177-1180(2003) 3.He, Y., Peng, S., Wang, J., et al.Ailanthone targets p23 to overcome MDV3100 resistance in castration-resistant prostate cancerNat. Commun.7:13122(2016)
Cell experiment: |
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 experiment: |
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]. |
References: [1]. He Y, et al. Ailanthone targets p23 to overcome MDV3100 resistance in castration-resistant prostate cancer. Nat Commun. 2016 Dec 13;7:13122. |
Cas No. | 981-15-7 | SDF | |
别名 | 臭椿酮,Δ13-Dehydrochaparrinone | ||
Canonical 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 | ||
分子式 | C20H24O7 | 分子量 | 376.4 |
溶解度 | DMSO : 83.3 mg/mL (221.31 mM) | 储存条件 | Store at 4°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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