Catalog No.S7326 Synonyms: LY573636
Molecular Weight(MW): 415.11
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)|
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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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