Adjudin
(Synonyms: 男用口服避孕药,AF-2364) 目录号 : GC19021
A derivative of lonidamine
Cas No.:252025-52-8
Sample solution is provided at 25 µL, 10mM.
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Adjudin is an extensively studied male contraceptive with a superior mitochondria-inhibitory effect. Adjudin is also a potent Cl- channel blocker.
Adjudin is a potent blocker of Cl- channels: disrupting Cl- ion transport function results in a decline in sperm capacitation and fertilizing ability in humans in vitro[1]. Adjudin (ADD) is a mitochondria inhibitor[2]. Adjudin is a molecule that mediates adherens junction disruption at the Sertoli-germ cell interface. To investigate the effect of Adjudin on cancer cells, more than ten different types of human or mice cancer cell lines are treated with increasing concentrations of Adjudin and the cell proliferation is measured by the modified MTT assay. Adjudin inhibits cell proliferation in a dose dependent manner in SGC-7901 (human gastric adenocarcinoma cell), MDA-MB-231 (human breast adenocarcinoma cell), Smmc-7721 (human hepatoma cell) and MIA Paca-2 (human pancreatic adenocarcinoma cell) cells. The IC50 of Adjudin is determined to be 58.0 uM, 13.8 uM, 72.3 uM and 52.7 uM against SGC-7901, MDA-MB-231, Smmc-7721 and MIA Paca-2 cells, respectively, after treatment for 24 h. Similar results are obtained in other human and mice cancer cell lines. The IC50 of Adjudin in A549 cells and PC3 cells is 63.1 uM and 93.0 uM, respectively. For WI-38 and BPH-1 cells, the IC50 of Adjudin can be observed at more than 300 uM and 200 uM, respectively, which is about 5 times and 2 times more than that for the cancer cell lines A549 and PC3[3].
To determine whether Adjudin can inhibit lung and prostate cancer growth in vivo, the effect of Adjudin is tested in a subcutaneous model of lung and prostate cancer. Human lung carcinoma cells A549 and prostate carcinoma cells PC3 are injected into athymic nude mice subdermally at the lower back site respectively. Mice are then randomized into two treatment groups with similar mean tumor sizes: Adjudin and vehicle (control). Approximately 2 weeks after tumor inoculation Adjudin is injected intraperitoneally once every three days in lung carcinoma cells and every other day in prostate carcinoma cells at 100 mg/kg. Adjudin treatment can be well tolerated in rodent. And Adjudin-treated mice show significant tumor growth inhibition compared with the control group (P<0.0001 in the human lung carcinoma cells A549 and P=0.006 in the prostate carcinoma cells PC3)[3].
References:
[1]. Li K, et al. Inhibition of sperm capacitation and fertilizing capacity by adjudin is mediated by chloride and its channels in humans. Hum Reprod. 2013 Jan;28(1):47-59.
[2]. Li X, et al. Combination delivery of Adjudin and Doxorubicin via integrating drug conjugation and nanocarrier approaches for the treatment of drug-resistant cancer cells. J Mater Chem B. 2015 Feb 28;3(8):1556-1564.
[3]. Xie QR, et al. Male contraceptive Adjudin is a potential anti-cancer drug. Biochem Pharmacol. 2013 Feb 1;85(3):345-55.
Cell experiment: | A549 cells, WI-38 cells, BPH-1 cells, PC-12 cells and other cell lines are seeded in 96-well plates at the density of 0.5×104/well in the complete growth medium and incubated for 24 h. Then the growth medium is replaced with a serial dilution of Adjudin (300 µM, 100 µM, 30 µM, 10 µM, 3 µM and 0) in growth medium (without serum). The cells are incubated for another 24 h followed by the addition of 10 µl of Cell Counting Kit-8 solution to each well. After 4 h of incubation at 37 °C in the cell incubator, the absorbance at 450 nm is measured using a microplate reader[3]. |
Animal experiment: | Mice[3]The male BALB/C nude mice weighing ~20g are equally implanted with A549 cells (0.5×107 cells) containing 3 mg/mL of matrigel and PC3 cells (1×106 cells) hypodermically. After 2 weeks, the mice with palpable tumors are divided into two groups (n=4 per group in each experiment and repeated with a total of three experiments): i.p. injection of Adjudin which is dissolved in corn oil from a DMSO stock solution with final administered quantity at 100 mg/kg (~300 µM used in vitro); the equivalent vehicle control group are administered with the same amount of corn oil and DMSO via i.p. injection. Adjudin or vehicles are administered every three day in A549 and every other day in PC3 up to 2 weeks. Tumor volumes are determined and calculated. |
References: [1]. Li K, et al. Inhibition of sperm capacitation and fertilizing capacity by adjudin is mediated by chloride and its channels in humans. Hum Reprod. 2013 Jan;28(1):47-59. | |
| Cas No. | 252025-52-8 | SDF | |
| 别名 | 男用口服避孕药,AF-2364 | ||
| Canonical SMILES | O=C(C1=NN(CC2=CC=C(Cl)C=C2Cl)C3=C1C=CC=C3)NN | ||
| 分子式 | C15H12Cl2N4O | 分子量 | 335.19 |
| 溶解度 | DMSO : ≥ 34 mg/mL (101.44 mM) | 储存条件 | Store at -20°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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9834 mL | 14.9169 mL | 29.8338 mL |
| 5 mM | 0.5967 mL | 2.9834 mL | 5.9668 mL |
| 10 mM | 0.2983 mL | 1.4917 mL | 2.9834 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet