Tasisulam
(Synonyms: 他斯索兰,LY 573636) 目录号 : GC10294
An anticancer agent
Cas No.:519055-62-0
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 519055-62-0 | SDF | |
| 别名 | 他斯索兰,LY 573636 | ||
| 化学名 | N-(5-bromothiophen-2-yl)sulfonyl-2,4-dichlorobenzamide | ||
| Canonical SMILES | C1=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 tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.409 mL | 12.045 mL | 24.09 mL |
| 5 mM | 0.4818 mL | 2.409 mL | 4.818 mL |
| 10 mM | 0.2409 mL | 1.2045 mL | 2.409 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet