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| 500mg | ||
| 1g | ||
| Other Sizes |
Tasisulam sodium (LY573636 Na), an acyl-sulfonamide analog, is a potent anticancer/tumor agent that is able to induce tumor cell apoptosis by a mitochondrial-targeted mechanism involving the loss of mitochondrial membrane potential and induction of reactive oxygen species (ROS). It acts as an apoptosis inducer and caspase activator.
| ln Vitro |
Inducing antiproliferative responses in various tumor histologies, tesisulamodium (200 nM-200 μM; 48 hours) has EC50s of 10 μM and 25 μM for Calu-6 and A-375 cell lines, respectively [1]. 4N DNA and G2-M accumulation increase in a concentration-dependent manner when exposed to tasisulam sodium (25, 50 μM; 72 hours) [1]. Numerous in vitro cancer cell types undergo apoptosis when exposed to tesisulam sodium (200 nM–200 μM; 48 hours) [1]. Tasisulam sodium also inhibits the production of endothelial cords that are stimulated by fibroblast growth factor, epidermal growth factor, and VEGF [1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: Calu-6 Non-Small Cell Lung Cancer and A-375 Melanoma Model Tested Concentrations: 200 nM-200 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induction of anti-proliferative responses in multiple tumor histologies EC50 respectively are 10 μM and 25 μM. Cell cycle analysis [1] Cell Types: Calu-6 and A-375 cell lines Tested Concentrations: 25, 50 μM Incubation Duration: 72 hrs (hours) Experimental Results: Induced concentration-dependent increase in 4N DNA and G2-M accumulation. Apoptosis analysis[1] Cell Types: Calu-6 non-small cell lung cancer and A-375 melanoma models Tested Concentrations: 200 nM-200 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induction of apoptosis in multiple in vitro cancer cell models . |
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| Animal Protocol |
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| References |
[1]. Meier T, et al. Tasisulam sodium, an antitumor agent that inhibits mitotic progression and induces vascular normalization. Mol Cancer Ther. 2011 Nov;10(11):2168-78.
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| Additional Infomation |
Tasisulam Sodium is the sodium salt of an acyl-sulfonamide with potential antineoplastic activity. Selectively toxic towards tumor cells, tasisulam appears to induce tumor cell apoptosis by a mitochondrial-targeted mechanism involving the loss of mitochondrial membrane potential and induction of reactive oxygen species (ROS). In combination with an angiogenesis inhibitor, this agent may exhibit synergistic antiangiogenic activity.
See also: Tasisulam (annotation moved to). |
| Molecular Formula |
C11H6NO3S2CL2BR
|
|---|---|
| Molecular Weight |
415.11024
|
| Exact Mass |
434.817
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| CAS # |
519055-63-1
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| Related CAS # |
Tasisulam;519055-62-0
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| PubChem CID |
23718384
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| Appearance |
Typically exists as solid at room temperature
|
| LogP |
5.464
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
21
|
| Complexity |
477
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C=CC(C(NS(C2=CC=C(Br)S2)(=O)=O)=O)=C(Cl)C=1
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| InChi Key |
JCOHXVDKRMWUQP-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C11H6BrCl2NO3S2.Na/c12-9-3-4-10(19-9)20(17,18)15-11(16)7-2-1-6(13)5-8(7)14;/h1-5H,(H,15,16);/q;+1/p-1
|
| Chemical Name |
sodium;(5-bromothiophen-2-yl)sulfonyl-(2,4-dichlorobenzoyl)azanide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4090 mL | 12.0450 mL | 24.0900 mL | |
| 5 mM | 0.4818 mL | 2.4090 mL | 4.8180 mL | |
| 10 mM | 0.2409 mL | 1.2045 mL | 2.4090 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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