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Purity: ≥98%
Tasisulam (LY-573636), 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). Additionally, it activates caspases and induces apoptosis.
| Targets |
Caspase
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| ln Vitro |
Tasisulam has an ED50 range of 7 to 40 M and inhibits the growth of several human leukemia and lymphoma cell lines. In HL60, Reh, and MD901 cells, LY573636 also causes apoptosis, primarily through the loss of mitochondrial membrane potential and the induction of reactive oxygen species. [1] Additionally, Tasisulam exhibits antiproliferative effects in over 70% of the 120 tested cell lines with an EC50 of less than 50 μM. In Calu-6 and A-375 cells, tasisulam causes G2-M accumulation and subsequently apoptosis. Tasisulam also blocks endothelial cord formation brought on by VEGF, FGF, and EGF in vitro, with EC50 values of 47, 103, and 34 nM, respectively.[2]
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| ln Vivo |
Tasisulam causes decreased hypoxia and increased pericyte coverage in vivo, which are morphologic characteristics of vascular normalization. In the Calu-6 non-small cell lung xenograft model, tasisulam (25 or 50 mg/kg, i.v.) induces apoptosis, exhibits dose-dependent antitumor activity, and normalizes tumor-associated vasculature. Additionally, Tasisulam exhibits strong antitumor activity against a variety of in vivo xenografts, such as colorectal (HCT-116), melanoma (A-375), gastric (NUGC-3), leukemia (MV-4-11), and pancreatic (QGP-1). [2]
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| Cell Assay |
In order to perform the 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, cells are exposed to LY573636 at various concentrations. In a nutshell, 5 mg/mL of MTT is dissolved in phosphate-buffered saline (PBS). In 96-well plates, 1,000 cells per well are cultured in medium for 96 hours before 10 μL of the MTT solution is added. 100 μL of solubilization solution (20% sodium dodecyl sulfate [SDS]) is added after a 4-hour incubation, and the mixture is then incubated at 37 °C for 16 hours. In this assay, metabolically active cells cleave MTT into an orange formazan dye, and the formazan product's absorbance is measured with an enzyme-linked immunoabsorbent assay (ELISA) reader at 540 nm.
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| Animal Protocol |
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| References | ||||
| Additional Infomation |
Tasisulam has been used in trials studying the treatment and basic science of Melanoma, Lymphoma, Solid Tumors, Breast Cancer, and Ovarian Cancer, among others.
Tasisulam is 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. |
| Molecular Formula |
C11H6BRCL2NO3S2
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|---|---|
| Molecular Weight |
415.11
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| Exact Mass |
412.834
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| Elemental Analysis |
C, 31.83; H, 1.46; Br, 19.25; Cl, 17.08; N, 3.37; O, 11.56; S, 15.45
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| CAS # |
519055-62-0
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| Related CAS # |
Tasisulam sodium;519055-63-1
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| PubChem CID |
10160238
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.8±0.1 g/cm3
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| Index of Refraction |
1.657
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| LogP |
3.94
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
471
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NS(=O)(C1=CC=C(Br)S1)=O)C2=CC=C(Cl)C=C2Cl
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| InChi Key |
WWONFUQGBVOKOF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H6BrCl2NO3S2/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)
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| Chemical Name |
N-(5-bromothiophen-2-yl)sulfonyl-2,4-dichlorobenzamide
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| Synonyms |
Tasisulam sodium; Tasisulam; LY573636; LY 573636; LY-573636
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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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00383292 | Completed | Drug: tasisulam | Metastatic Melanoma | Eli Lilly and Company | November 2006 | Phase 2 |
| NCT01209832 | Terminated | Drug: Tasisulam Drug: Midazolam |
Advanced Cancer | Eli Lilly and Company | September 2010 | Phase 1 |
| NCT01185548 | Terminated | Drug: Tolbutamide Drug: Tasisulam |
Lymphoma Advanced Cancer |
Eli Lilly and Company | July 2010 | Phase 1 |
| NCT01006252 | Terminated | Drug: Tasisulam-sodium Drug: Paclitaxel |
Melanoma | Eli Lilly and Company | December 2009 | Phase 3 |
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