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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01209832 Terminated Drug: Tasisulam|Drug: Midazolam Advanced Cancer Eli Lilly and Company September 2010 Phase 1
NCT01214668 Completed Drug: LY573636-sodium|Drug: Liposomal Doxorubicin Solid Tumors Eli Lilly and Company January 2009 Phase 1
NCT00718159 Completed Drug: LY573636-sodium Acute Myeloid Leukemia|Essential Thrombocythemia Eli Lilly and Company August 2008 Phase 1
NCT01258348 Completed Drug: Drug: LY573636-sodium|Drug: Sunitinib Metastatic Renal Cell Cancer Eli Lilly and Company July 2008 Phase 1
NCT01215916 Completed Drug: LY573636|Drug: Pemetrexed Solid Tumors Eli Lilly and Company February 2008 Phase 1
NCT00490451 Completed Drug: LY573636-sodium Sarcoma Soft Tissue Eli Lilly and Company August 2007 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID