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Tasisulam Caspase activator

Cat.No.S7326

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

Chemical Structure

Molecular Weight: 415.11

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 415.11 Formula

C11H6BrCl2NO3S2

 Storage (From the date of receipt)
CAS No. 519055-62-0 Download SDF Storage of Stock Solutions

Synonyms LY573636 Smiles C1=CC(=C(C=C1Cl)Cl)C(=O)NS(=O)(=O)C2=CC=C(S2)Br

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (199.94 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 83 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
Caspase [1]
In vitro
Tasisulam inhibits growth of various human leukemia and lymphoma cell lines with ED50 ranging from 7 to 40 μM. This compound 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, this chemical also produce antiproliferative activities in more than 70% of the 120 cell lines tested with EC50 of less than 50 μM. It induces G2–M accumulation and subsequent apoptosis in Calu-6 and A-375 cells. In vitro, this agent 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. This compound (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, it 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]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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