Home Apoptosis Caspase activator Tasisulam For research use only.

Tasisulam

Synonyms: LY573636

Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.

Tasisulam Chemical Structure

Tasisulam Chemical Structure

CAS No. 519055-62-0

Purity & Quality Control

Batch: S732601 DMSO]83 mg/mL]false]Ethanol]83 mg/mL]false]Water]Insoluble]false Purity: 99.93%
99.93

Tasisulam Related Products

Signaling Pathway

Caspase Signaling Pathways

Caspase Signaling Pathway

Biological Activity

Description Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.
Targets
Caspase [1]
In vitro
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Calu-6 non–small cell lung xenograft model
Dosages ~50 mg/kg
Administration i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01209832 Terminated
Advanced Cancer
Eli Lilly and Company
 September 2010 Phase 1
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
NCT01258348 Completed
Metastatic Renal Cell Cancer
Eli Lilly and Company
 July 2008 Phase 1
NCT01215916 Completed
Solid Tumors
Eli Lilly and Company
 February 2008 Phase 1
NCT00490451 Completed
Sarcoma Soft Tissue
Eli Lilly and Company
 August 2007 Phase 2

Chemical Information & Solubility

Molecular Weight 415.11 Formula

C11H6BrCl2NO3S2
CAS No. 519055-62-0 SDF Download Tasisulam SDF
Smiles C1=CC(=C(C=C1Cl)Cl)C(=O)NS(=O)(=O)C2=CC=C(S2)Br
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 83 mg/mL ( (199.94 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 83 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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