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Tasisulam
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tasisulam图片
CAS NO:519055-62-0
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Tasisulam 是一种抗癌剂,通过内在途径诱导细胞凋亡,导致细胞色素 c 释放和半胱天冬酶依赖性细胞死亡。 Tasisulam 抑制有丝分裂进程并诱导血管正常化。
Cas No.519055-62-0
别名他斯索兰,LY 573636
化学名N-(5-bromothiophen-2-yl)sulfonyl-2,4-dichlorobenzamide
Canonical SMILESC1=CC(=C(C=C1Cl)Cl)C(=O)NS(=O)(=O)C2=CC=C(S2)Br
分子式C11H6BrCl2NO3S2
分子量415.11
溶解度≥ 20.3mg/mL in DMSO
储存条件Store at -20° C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Tasisulam is an antitumor agent [1].

Tasisulam is an antitumor agent that induced growth arrest and apoptosis of human solid tumours. In human malignant hematopoietic cell lines, tasisulam inhibited cells growth with ED50 values of 5, 7, 12, 13, 21 and 31 μM for BALL1, HL60, RCH, NCEB1, SP49 and Daudi cell lines, respectively. Tasisulam induced growth arrest in a dose-dependent way. Also, tasisulam caused induction of ROS, loss of mitochondrial membrane potential and induction of apoptosis. In HL60 and U937 cells, tasisulam induce granulocytic/monocytic differentiation. In solid tumor cell lines, tasisulam induced apoptosis that was mediated by the mitochondrial-mediated cell death pathways [1]. Tasisulam increased phospho-histone H3 expression and cells with 4N DNA, and led to G2-M accumulation and apoptosis. Tasisulam also inhibited endothelial cell cord formation induced by epidermal growth factor, VEGF and fibroblast growth factor with EC50 values of 34, 47 and 103 nM, respectively.

In mice bearing the Calu-6 non-small cell lung xenograft model, tasisulam exhibited antitumor efficacy in a dose-dependent way and reduced tumor volume by 77%. Tasisulam caused G2-M accumulation and increased nuclear fragmentation. Also, tasisulam induced vascular normalization [2].

References:
[1].  Haritunians T, Gueller S, O'Kelly J, et al. Novel acyl sulfonamide LY573636-sodium: effect on hematopoietic malignant cells. Oncol Rep, 2008, 20(5): 1237-1242.
[2].  Meier T, Uhlik M, Chintharlapalli S, et al. Tasisulam sodium, an antitumor agent that inhibits mitotic progression and induces vascular normalization. Mol Cancer Ther, 2011, 10(11): 2168-2178.