Adjudin (Synonyms: AF-2364) |
| Catalog No.GC19021 |
Adjudin is an extensively studied male contraceptive with a superior mitochondria-inhibitory effect.
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Synonyms | AF-2364 | ||
| Canonical SMILES | O=C(C1=NN(CC2=CC=C(Cl)C=C2Cl)C3=C1C=CC=C3)NN | ||
| Formula | C15H12Cl2N4O | M.Wt | 335.19 |
| Solubility | DMSO : ≥ 34 mg/mL (101.44 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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