Tasisulam

Catalog No.S7326 Synonyms: LY573636

Tasisulam Chemical Structure

Molecular Weight(MW): 415.11

Tasisulam is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.

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Biological Activity

Description Tasisulam is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.
Targets
Caspase [1]
In vitro

Tasisulam inhibits growth of various human leukemia and lymphoma cell lines with ED50 ranging from 7 to 40 μM. LY573636 also induces apoptosis in HL60, Reh, and MD901 cells, mainly by loss of mitochondrial membrane potential and induction of reactive oxygen species. [1] In addition, Tasisulam also produce antiproliferative activities in more than 70% of the 120 cell lines tested with EC50 of less than 50 μM. Tasisulam induces G2–M accumulation and subsequent apoptosis in Calu-6 and A-375 cells. In vitro, Tasisulam also inhibits VEGF-, FGF- and EGF-induced endothelial cord formation with EC50 of 47, 103, and 34 nM, respectively. [2]
In vivo Tasisulam induces morphologic features of vascular normalization, including increased pericyte coverage and decreased hypoxia in vivo. Tasisulam (25 or 50 mg/kg, i.v.) displays dose-dependent antitumor activity, induces apoptosis, and normalizes tumor-associated vasculature in the Calu-6 non–small cell lung xenograft model. Besides, Tasisulam displays potent antitumor activity across a range of in vivo xenografts, including colorectal (HCT-116), melanoma (A-375), gastric (NUGC-3), leukemia (MV-4-11), and pancreatic (QGP-1). [2]

Protocol

Cell Research:

[1]
+ Expand
  • Cell lines: B-cell acute lymphocytic leukemia (Reh, RCH, BALL1), Burkitt’s lymphoma (Daudi), diffuse large B-cell lymphoma (MD901, LY4), myeloid leukemia cell lines (HL60 and U937), Mantle cell lymphoma cell lines (NCEB1, Jeko1, and SP49).
  • Concentrations: ~40 μM
  • Incubation Time: 96 hours
  • Method:

    Cells are treated with various concentrations of LY573636. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay is performed. Briefly, MTT is dissolved in phosphate-buffered saline (PBS) at 5 mg/mL. Approximately 1,000 cells per well are incubated in culture medium for 96 hours in 96-well plates; and then, 10 μL of the MTT solution is added. After a 4-hour incubation, 100 μL of solubilization solution (20 % sodium dodecyl sulfate [SDS]) is added, and the mixture was incubated at 37 °C for 16 hours. In this assay, MTT is cleaved to an orange formazan dye by metabolically active cells; and the absorbance of the formazan product is measured with an enzyme-linked immunoabsorbent assay (ELISA) reader at 540 nm.


    (Only for Reference)
Animal Research:

[2]
+ Expand
  • Animal Models: Calu-6 non–small cell lung xenograft model
  • Formulation: Physiologic saline
  • Dosages: ~50 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL (199.94 mM)
Ethanol 83 mg/mL (199.94 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 415.11
Formula

C11H6BrCl2NO3S2
CAS No. 519055-62-0
Storage powder
in solvent
Synonyms LY573636

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01209832 Terminated Advanced Cancer Eli Lilly and Company September 2010 Phase 1
NCT01185548 Terminated Lymphoma|Advanced Cancer Eli Lilly and Company July 2010 Phase 1
NCT01006252 Terminated Melanoma Eli Lilly and Company December 2009 Phase 3
NCT00992225 Completed Breast Cancer Eli Lilly and Company September 2009 Phase 2
NCT01214668 Completed Solid Tumors Eli Lilly and Company January 2009 Phase 1
NCT00718159 Completed Acute Myeloid Leukemia|Essential Thrombocythemia Eli Lilly and Company August 2008 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Caspase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID