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产品描述:

产品名称:Tasisulam

靶点: Caspase

CAS号: 519055-62-0

描述: Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization.

中文别名: 他斯索兰

英文别名: LY 573636

外观: Powder

In vitro(体外研究): 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.

分子式: C₁₁H₆BrCl₂NO₃S₂

In vivo(体内研究): 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).

分子量: 415.11

纯度: >98%

储存/保存方法: store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.

可溶性/溶解性: DMSO : 250 mg/mL (602.25 mM; Need ultrasonic)

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