他司磺胺|T6191|TargetMol

Tasisulam
519055-62-0

￥149 1mg 起订

￥332 5mg 起订

￥533 10mg 起订

上海更新日期：2024-09-29

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产品详情:

中文名称：: 他司磺胺

英文名称：: Tasisulam

CAS号：: 519055-62-0

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.97%

产品类别：: 抑制剂

货号：: T6191

Product Introduction

Bioactivity

Name	Tasisulam
Description	Tasisulam (LY573636) is an apoptosis inducer and an antitumor agent via the intrinsic pathway.
Cell Research	Cells are treated with various concentrations of LY573636. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay is performed. Briefly, MTT is dissolved in phosphate-buffered saline (PBS) at 5 mg/mL. Approximately 1,000 cells per well are incubated in culture medium for 96 hours in 96-well plates; and then, 10 μL of the MTT solution is added. After a 4-hour incubation, 100 μL of solubilization solution (20 % sodium dodecyl sulfate [SDS]) is added, and the mixture was incubated at 37 °C for 16 hours. In this assay, MTT is cleaved to an orange formazan dye by metabolically active cells; and the absorbance of the formazan product is measured with an enzyme-linked immunoabsorbent assay (ELISA) reader at 540 nm. (Only for Reference)
Kinase Assay	Electrophysiology: The human IKCa1 is cloned and expressed in COS-7 cells. Cells are studied in the whole-cell configuration of the patch-clamp technique. The holding potential is 280 mV. The internal pipette solution contains: 145 mM K+ aspartate, 2 mM MgCl2, 10 mM Hepes, 10 mM K2EGTA, and 8.5 mM CaCl2 (1 μM free Ca2+), pH 7.2, 290-310 mOsm. To reduce currents from the native chloride channels in COS-7 cells, Na+ aspartate Ringer is used as an external solution: 160 mM Na+ aspartatey/4.5 mM KCl/2 mM CaCl2/1 mM MgCl2/5 mM Hepes, pH 7.4/290-310 mOsm. IKCa currents in COS-7 cells are elicited by 200-ms voltage ramps from -120 mV to 40 mV applied every 10 seconds and the reduction of slope conductance at -80 mV by TRAM-34 taken as a measure of channel block.
In vitro	Tasisulam在多种人类白血病和淋巴瘤细胞系中抑制生长，ED50值介于7至40μM之间。LY573636还通过丧失线粒体膜电位和诱导活性氧种类的产生，在HL60、Reh和MD901细胞中诱导凋亡。[1]此外，Tasisulam在测试的120种细胞系中70%以上显示出抗增殖活性，EC50值小于50μM。Tasisulam在Calu-6和A-375细胞中诱导G2-M堆积及随后的凋亡。在体外，Tasisulam还能抑制由VEGF、FGF和EGF诱导的内皮细胞索形成，其EC50值分别为47、103和34nM。[2]
In vivo	Tasisulam在活体内诱导血管正常化的形态特征，包括提高脉络膜细胞覆盖率和降低低氧状态。Tasisulam（25或50 mg/kg, i.v.）显示出剂量依赖性的抗肿瘤活性，能够诱导凋亡并正常化与Calu-6非小细胞肺癌异种移植模型相关的血管。此外，Tasisulam在多种活体内异种移植模型中显示出强大的抗肿瘤活性，包括结直肠癌（HCT-116）、黑色素瘤（A-375）、胃癌（NUGC-3）、白血病（MV-4-11）和胰腺癌（QGP-1）。[2]
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	Ethanol : 77 mg/mL (185.5 mM) DMSO : 77 mg/mL (185.5 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
Keywords	Apoptosis \| LY 573636 \| LY-573636 \| inhibit \| Inhibitor \| Tasisulam
Inhibitors Related	Stavudine \| L-Ascorbic acid \| Sodium 4-phenylbutyrate
Related Compound Libraries	Anti-Cancer Active Compound Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Drug Repurposing Compound Library \| Anti-Cancer Clinical Compound Library \| Anti-Cancer Drug Library

他司磺胺|||LY573636|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
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年营业额	￥ 1亿以上
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主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务