Bithionol (Synonyms: CP 3438, NSC 9872, NSC 47129) |
Catalog No.GC15976
One-Click Copy Product Info
|
potent inhibitor of soluble adenylyl cyclase (sAC)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 97-18-7
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
IC50: 19 μM – 60 μM for various ovarian cancer cell lines
Bithionol is a potent inhibitor of soluble adenylyl cyclase (sAC).
Adenylyl cyclase is an enzyme with critical regulatory roles in cells. All classes of adenylyl cyclases can catalyse the conversion of adenosine triphosphate to 3',5'-cyclic AMP and pyrophosphate.
In vitro: Bithionol could cause dose-dependent cytotoxicity toward all tested ovarian cancer cell lines regardless of their sensitivities to cisplatin. Moreover, such cell death appeared to be via caspases mediated apoptosis. In addition, the mechanism of action appeared to be partially by cell cycle arrest, ROS generation as well as ATX inhibition [1].
In vivo: Oral toxicity of bithionol sulfoxide was assessed in acute toxicity studies in mice and rats. The median lethal dose (LD50) values in mice were > 1000 mg/kg and < 5000 mg/kg after 21 days; the male rat LD50 value was around 5000 mg/kg after 48 h. Moreover, the hepatic toxicity was observed at all tested doses. Increases in serum AST were observed with the high doses, suggesting that mitochondria were affected. In addition, the histological study indicated more intense periportal fatty infiltration with high doses at 5000 and 500 mg/kg [2].
Clinical trial: In a previous study, bithionol was orally given to patients with acute fascioliasis at the daily dose of 25 mg/kg for 10 days. Results showed that all patients were cured. The follow-up period after the first course of treatment was between 16 and 47 months and no major side effects were found [3].
References:
[1] Ayyagari VN,Brard L. Bithionol inhibits ovarian cancer cell growth in vitro - studies on mechanism(s) of action. BMC Cancer.2014 Feb 4;14:61.
[2] Lavric A, Skubic V, Senk L, Lukanc G, Kacl E. Oral toxicity of bithionol sulfoxide in mice and rats. Zbornik Veterinarske Fakultete Univerza Ljubljana 1990 27(1): 33-39
[3] Bacq Y,Besnier JM,Duong TH,Pavie G,Metman EH,Choutet P. Successful treatment of acute fascioliasis with bithionol. Hepatology.1991 Dec;14(6):1066-9.
| Cas No. | 97-18-7 | SDF | |
| Synonyms | CP 3438, NSC 9872, NSC 47129 | ||
| Chemical Name | 6,6'-thiobis(2,4-dichlorophenol) | ||
| Canonical SMILES | ClC1=CC(Cl)=C(O)C(SC2=CC(Cl)=CC(Cl)=C2O)=C1 | ||
| Formula | C12H6Cl4O2S | M.Wt | 356.05 |
| Solubility | DMSO: 20mg/mL | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8086 mL | 14.043 mL | 28.0859 mL |
| 5 mM | 561.7 μL | 2.8086 mL | 5.6172 mL |
| 10 mM | 280.9 μL | 1.4043 mL | 2.8086 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 saline, 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
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)