Tasisulam (LY573636)

Alias: Tasisulam sodium; Tasisulam; LY573636; LY 573636; LY-573636
Cat No.:V0027 Purity: ≥98%
Tasisulam(LY-573636), anacyl-sulfonamide analog,is a potent anticancer/tumor agent that is able toinduce tumor cell apoptosis by a mitochondrial-targeted mechanism involving the loss of mitochondrial membrane potential and induction of reactive oxygen species (ROS).
Tasisulam (LY573636) Chemical Structure CAS No.: 519055-62-0
Product category: Caspase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
Other Sizes

Other Forms of Tasisulam (LY573636):

  • Tasisulam sodium
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
Targets
Caspase
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]
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]
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.
Animal Protocol
50 mg/kg
saline
Calu-6 non–small cell lung xenograft model
References

[1]. Oncol Rep . 2008 Nov;20(5):1237-42.

[2]. Mol Cancer Ther . 2011 Nov;10(11):2168-78.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H6BRCL2NO3S2
Molecular Weight
415.11
Exact Mass
412.84
Elemental Analysis
C, 31.83; H, 1.46; Br, 19.25; Cl, 17.08; N, 3.37; O, 11.56; S, 15.45
CAS #
519055-62-0
Appearance
Solid powder
SMILES
C1=CC(=C(C=C1Cl)Cl)C(=O)NS(=O)(=O)C2=CC=C(S2)Br
InChi Key
WWONFUQGBVOKOF-UHFFFAOYSA-N
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)
Chemical Name
N-(5-bromothiophen-2-yl)sulfonyl-2,4-dichlorobenzamide
Synonyms
Tasisulam sodium; Tasisulam; LY573636; LY 573636; LY-573636
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO: ~83 mg/mL (~199.9 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: N/A
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

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.

Clinical Trial Information
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
Biological Data
  • Tasisulam

    In vitro effects of tasisulam on endothelial and adipose-derived stem cells.Mol Cancer Ther.2011 Nov;10(11):2168-78.
  • Tasisulam
    Effects of tasisulam on blood vessel formation in vivo.Mol Cancer Ther.2011 Nov;10(11):2168-78.
  • Tasisulam

    Tasisulam displays dose-dependent antitumor activity, induces apoptosis, and normalizes tumor-associated vasculature in the Calu-6 non–small cell lung xenograft model.Mol Cancer Ther.2011 Nov;10(11):2168-78.
Contact Us