化合物 S3I-201|T2505

價格	￥415	￥583	￥1465
包裝	5mg	10mg	50mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-14

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產(chǎn)品詳情

中文名稱:化合物 S3I-201	英文名稱:S3I-201
CAS:501919-59-1	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.05%	產(chǎn)品類別: 抑制劑
貨號: T2505

Product Introduction

Bioactivity

名稱	S3I-201
描述	S3I-201 (S3I-201) is a selective Stat3 inhibitor (IC50: 86±33 μM) and low effect towards STAT1/5.
細(xì)胞實驗	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].
激酶實驗	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].
動物實驗	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].
體外活性	S3I-201抑制Stat3和Stat3復(fù)合體的形成以及Stat3的DNA結(jié)合和轉(zhuǎn)錄活性。此外，S3I-201主要在含有持續(xù)活化Stat3的腫瘤細(xì)胞中抑制生長并誘導(dǎo)凋亡。構(gòu)成性二聚和活性Stat3C以及Stat3 SH2結(jié)構(gòu)域可使腫瘤細(xì)胞免受S3I-201引起的凋亡[1]。在p53(null)CD45.1小鼠的CD4 T細(xì)胞中，先用不同濃度的S3I-201預(yù)處理，可以在添加IL-6后最早15分鐘抑制STAT3的磷酸化，呈劑量依賴性。根據(jù)STAT3磷酸化抑制水平，確定此抑制劑的IC50為38μM [2]。雖然這些細(xì)胞系對單獨使用S3I-201（S3I-201）不敏感，但S3I-201增強了所有三個細(xì)胞系（HepG2、SK-HEP1和Huh-7細(xì)胞）對cetuximab的抗增殖效果[3]。
體內(nèi)活性	與對照組瘤體相比，接受S3I-201治療的小鼠中的人類乳腺癌瘤顯示出強烈的生長抑制作用。與對照組瘤體相比，S3I-201處理的小鼠殘留腫瘤組織中Stat3 DNA結(jié)合活性受到強烈抑制。使用PBS處理的同齡p53nullCD45.1小鼠作為對照組，對8至10周齡的p53nullCD45.1小鼠每周3次以5 mg/kg劑量治療S31-201。與PBS處理的小鼠相比，S31-201處理的小鼠脾臟中的STAT3磷酸化顯著降低。S3I-201減輕了大鼠異種移植模型中的生長激素分泌和腺垂體瘤生長。
存儲條件	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)
關(guān)鍵字	Inhibitor \| inhibit \| NSC74859 \| STAT \| NSC 74859 \| NSC-74859
相關(guān)產(chǎn)品	Nifuroxazide \| Diosgenin \| Niclosamide olamine \| Balsalazide sodium hydrate

關(guān)鍵字： S3I 201|||S3I201|TargetMol

公司簡介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個性化定制合成；從對明確靶點的分子篩選到對明確分子的多靶點篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國市場五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊資本	566.2651萬人民幣
員工人數(shù)	100-500人	年營業(yè)額	￥ 1億以上
主營行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國（陶術(shù)生物）

VIP 12年

公司成立：12年
注冊資本：566.2651萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑，藥物篩選化合物庫，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場三路28號4樓

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