Tasisulam
For research use only.
Catalog No.S7326 Synonyms: LY573636
1 publication

CAS No. 519055-62-0
Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.
Selleck's Tasisulam has been cited by 1 publication
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Biological Activity
Description | Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3. | |
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Targets |
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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] |
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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: |
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Animal Research: |
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Solubility (25°C)
In vitro | DMSO | 83 mg/mL (199.94 mM) |
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Water | Insoluble | |
Ethanol | '83 mg/mL |
* 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 |
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Formula | C11H6BrCl2NO3S2 |
CAS No. | 519055-62-0 |
Storage |
powder in solvent |
Synonyms | LY573636 |
Smiles | C1=CC(=C(C=C1Cl)Cl)C(=O)NS(=O)(=O)C2=CC=C(S2)Br |
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
Dosage | mg/kg | Average weight of animals | g | Dosing volume per animal | ul | Number of animals | ||||
Step 2: Enter the in vivo formulation () | ||||||||||
% DMSO % % Tween 80 % ddH2O | ||||||||||
CalculateReset |
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: : mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL,)
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.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
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Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (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.
Molarity Calculator
Clinical Trial Information
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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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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