For research use only.
Catalog No.S7326 Synonyms: LY573636
CAS No. 519055-62-0
Tasisulam is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.
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|Description||Tasisulam is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.|
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.  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. 
|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). |
|In vitro||DMSO||83 mg/mL (199.94 mM)|
|Ethanol||83 mg/mL (199.94 mM)|
* 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.
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|
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 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.
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
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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