An anticancer agent; inhibits the growth of Calu-6 NSCLC and A-375 melanoma cell lines (EC50s = 10 and 25 μM

Tasisulam – 25 mg

Brand:
Cayman
CAS:
519055-62-0
Storage:
-20
UN-No:
Non-Hazardous - /

Tasisulam is an anticancer agent that inhibits the growth of Calu-6 non-small cell lung carcinoma (NSCLC) and A-375 melanoma cell lines (EC50s = 10 and 25 μM, respectively).{39589} It arrests the cell cycle at the G2/M phase and induces apoptosis of Calu-6 cells in a concentration-dependent manner. Tasisulam induces non-apoptotic growth arrest in human vascular endothelial cells (HUVECs) and inhibits VEGF-, FGF-, and EGF-induced endothelial cord formation in vitro (EC50s = 47, 103, and 34 nM, respectively). In vivo, tasisulam (25 and 50 mg/kg) reduces hemoglobin content and blood vessel density in a Matrigel™ plug model of neoangiogenesis. It also reduces tumor growth in a dose-dependent manner in a Calu-6 mouse xenograft model via arrest of the cell cycle at the G2/M phase, induction of apoptosis, and reduction of tumor blood vessel density. Formulations containing tasisulam are under clinical investigation for the treatment of advanced solid tumors.  

 

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Description

An anticancer agent; inhibits the growth of Calu-6 NSCLC and A-375 melanoma cell lines (EC50s = 10 and 25 μM, respectively); induces arrests the cell cycle at the G2/M phase and induces apoptosis of Calu-6 cells in a concentration-dependent manner; induces non-apoptotic growth arrest in HUVECs and inhibits VEGF-, FGF-, and EGF-induced endothelial cord formation in vitro (EC50s = 47, 103, and 34 nM, respectively); reduces hemoglobin content and blood vessel density in a Matrigel™ plug model of neoangiogenesis; reduces tumor growth in a dose-dependent manner in a Calu-6 mouse xenograft model

Formal name: N-[(5-bromo-2-thienyl)sulfonyl]-2,4-dichloro-benzamide

Synonyms:  LY573636

Molecular weight: 415.1

CAS: 519055-62-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Death|Apoptosis

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