化合物 S3I-201|T2505

S3I-201
501919-59-1

￥415 5mg 起订

￥583 10mg 起订

￥1465 50mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 S3I-201

英文名称：: S3I-201

CAS号：: 501919-59-1

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：: 99.05%

产品类别：: 抑制剂

货号：: T2505

Product Introduction

Bioactivity

名称	S3I-201
描述	S3I-201 (S3I-201) is a selective Stat3 inhibitor (IC50: 86±33 μM) and low effect towards STAT1/5.
细胞实验	Proliferating cells were treated with or without S3I-201 for up to 48 h. In some cases, cells were first transfected with Stat3C, ST3-NT, or ST3-SH2 domain or mock-transfected for 24 h before treatment with compound for an additional 24–48 h. Cells were then detached and analyzed by annexin V binding according to the manufacturer's protocol and flow cytometry to quantify the percent apoptosis [1].
激酶实验	Briefly, 100 ml of biotinyl-e-Ac-EPQpYEEIEL-OH (in 50 mM Tris/150 mM NaCl, pH 7.5) was added to each well of streptavidin-coated 96-well microtiter plates and incubated with shaking at 4°C overnight. Then plates were rinsed with PBS/Tween 20 and then two times with 200 ml of BSA-T-PBS (0.2% BSA/0.1% Tween 20/PBS). Then 50 ml of Lck-SH2-GST fusion protein (6.4 ng/ml in BSA-T-PBS) was added to each well of the 96-well plate in the presence and absence of 50 ml of S3I-201 (for 30 and 100 mM final concentrations), and the plate was shaken at room temperature for 4 h. After solutions were removed, each well was rinsed four times with BSA-T-PBS (200 ml), and 100 ml of polyclonal rabbit anti-GST antibody (100 ng/ml in BSA-T-PBS) was added to each well and incubated at 4°C overnight. After washing with BSA-T-PBS, 100 ml of 200 ng/ml BSA-T-PBS horseradish peroxidase-conjugated mouse anti-rabbit antibody was added to each well and incubated for 45 min at room temperature. After four washing steps with BSA-T-PBS and three washing steps with PBS-T, 100 ml of peroxidase substrate was added to each well and incubated for 5-15 min. The peroxidase reaction was stopped by adding 100 ml of 1 M sulfuric acid solution, and absorbance was read at 450 nm with an ELISA plate reader [1].
动物实验	Six-week-old female athymic nude mice were purchased from Harlan and maintained in the institutional animal facilities approved by the American Association for Accreditation of Laboratory Animal Care. Athymic nude mice were injected in the left flank area s.c. with 5 × 10^6 human breast cancer MDA-MB-231 cells in 100 μl of PBS. After 5–10 days, tumors with a diameter of 3 mm were established. Animals were given S3I-201 i.v. at 5 mg/kg every 2 or 3 days for 2 weeks and monitored every 2 or 3 days. Animals were stratified so that the mean tumor sizes in all treatment were nearly identical. Tumor volume was calculated according to the formula V = 0.52 × a2× b, where a is the smallest superficial diameter and b is the largest superficial diameter [1].
体外活性	S3I-201抑制Stat3和Stat3复合体的形成以及Stat3的DNA结合和转录活性。此外，S3I-201主要在含有持续活化Stat3的肿瘤细胞中抑制生长并诱导凋亡。构成性二聚和活性Stat3C以及Stat3 SH2结构域可使肿瘤细胞免受S3I-201引起的凋亡[1]。在p53(null)CD45.1小鼠的CD4 T细胞中，先用不同浓度的S3I-201预处理，可以在添加IL-6后最早15分钟抑制STAT3的磷酸化，呈剂量依赖性。根据STAT3磷酸化抑制水平，确定此抑制剂的IC50为38μM [2]。虽然这些细胞系对单独使用S3I-201（S3I-201）不敏感，但S3I-201增强了所有三个细胞系（HepG2、SK-HEP1和Huh-7细胞）对cetuximab的抗增殖效果[3]。
体内活性	与对照组瘤体相比，接受S3I-201治疗的小鼠中的人类乳腺癌瘤显示出强烈的生长抑制作用。与对照组瘤体相比，S3I-201处理的小鼠残留肿瘤组织中Stat3 DNA结合活性受到强烈抑制。使用PBS处理的同龄p53nullCD45.1小鼠作为对照组，对8至10周龄的p53nullCD45.1小鼠每周3次以5 mg/kg剂量治疗S31-201。与PBS处理的小鼠相比，S31-201处理的小鼠脾脏中的STAT3磷酸化显著降低。S3I-201减轻了大鼠异种移植模型中的生长激素分泌和腺垂体瘤生长。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 40 mg/mL (109.48 mM)
关键字	Inhibitor \| inhibit \| NSC74859 \| STAT \| NSC 74859 \| NSC-74859
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S3I201|||S3I 201|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子