托法替尼|T6321

價(jià)格	￥297	￥483	￥813
包裝	5mg	10mg	25mg

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:托法替尼	英文名稱:Tofacitinib
CAS:477600-75-2	品牌: TargetMol
產(chǎn)地: 美國(guó)	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: 99.71%	產(chǎn)品類別: 抑制劑
貨號(hào): T6321

Product Introduction

Bioactivity

名稱	Tofacitinib
描述	Tofacitinib (Tasocitinib) is a Janus kinase inhibitor that inhibits JAK3/2/1 (IC50=1/20/112 nM) and is orally active. Tofacitinib is used for the treatment of moderate to severe rheumatoid arthritis.
細(xì)胞實(shí)驗(yàn)	To measure IL-2-dependent proliferation, isolated lymphocytes are resuspended to a cell density of 1-2 × 106/mL in complete RPMI medium (RPMI 1640 containing 10% (w/v) fetal calf serum (FCS), 1%(w/v) penicillin and treptomycin).Phytohemagluttinin (PHA) is added to a final concentration of 10 mg/mL, and the culture incubated for 3 days at 37 °C in a humidified 5% (v/v) CO2 incubator to upregulate IL-2R and JAK3 expression. IL-2 (200U/mL), with or without CP-690,550 is then added and the cells are incubated for 72 hours at 37 °C in a humidified 5% (v/v) CO2 incubator, after which 50 mL of 3H-thymidine (5mCi/mL) is added. The plates are incubated for an additional 18 hours, harvested with a 96-well harvester, and counted on a scintillation counter. HUO3 cells are maintained in culture with granulocyte-macrophage colony stimulating factor and human foreskin fibroblasts are maintained in culture with 10% fetal calf serum. CP-690550 is added to freshly plated cells and cultured for 4 days. 3Hthymidine is added during the last 18 hours of the culture period. (Only for Reference)
激酶實(shí)驗(yàn)	JAK3 Kinase Assay: A fragment encoding the catalytic domain of human JAK3 (785aa to 1125aa, JH1 catalytic domain) is amplified by PCR from the full length cDNA and cloned into the EcoRI site of the baculovirus transfer vector pVL1393. Recombinant baculovirus is used to infect Sf9 (Spodoptera frugipedra) cells and recombinant GSTJAK3 fusion protein is isolated on glutathione sepharose. The fusion protein is eluted with reduced glutathione and stored in buffer containing 50 mM Tris, pH 7.5, 10 mM DTT and 10% glycerol. JAK3 kinase activity is measured by ELISA as follows: Plates are coated overnight with a random L-glutamic acid and tyrosine co-polymer (4:1) (100 ug/mL). The plates are washed and recombinant JAK3 JH1:GST (100 ng/well) with or without inhibitors is incubated at room temperature for 30 minutes, after which HRP-conjugated PY20 anti-phosphotyrosine antibody (ICN) is added and developed by TMB (3,3',5,5'-tetramethylbenzidine). Other kinases (Table 1) are produced in E. coli or in insect cells, depending upon what is found to be optimal for the given kinase. The catalytic activity of tyrosine kinases is easured using the aftorementioned ELISA, whereas serine/threonine kinases are assayed using radioactive enzyme assays.
體外活性	方法: 人類 MM 細(xì)胞系 MM.1S 與永生化 BMSC 系 HS5 和 HS27A 共培養(yǎng)，用 Tofacitinib (0-10 μM) 處理 24 h，通過(guò) CellTiter-Glo reagent 檢測(cè)細(xì)胞活力。結(jié)果: 與單培養(yǎng)生長(zhǎng)相比，MM.1S 細(xì)胞數(shù)量顯著增加，證實(shí)了該細(xì)胞系中基質(zhì)誘導(dǎo)的增殖信號(hào)。Tofacitinib 處理以劑量依賴的方式減少了 MM.1S 細(xì)胞數(shù)量。Tofacitinib 單獨(dú)對(duì) MM.1S 細(xì)胞存活率或單獨(dú)對(duì)基質(zhì)細(xì)胞沒(méi)有影響。[1] 方法: NK-92 細(xì)胞用 Tofacitinib (50 nM) 處理過(guò)夜，再用 IL-15 (2.33 nM) 處理 2 h，檢測(cè) STAT1 磷酸化。結(jié)果: Tofacitinib 阻斷 NK-92 細(xì)胞中的 IL-15 信號(hào)傳導(dǎo)。Tofacitinib 通過(guò)阻斷 STAT 蛋白磷酸化來(lái)破壞 JAK/STAT 信號(hào)傳導(dǎo)。[2]
體內(nèi)活性	方法: 為檢測(cè)體內(nèi)抗腫瘤活性，用 Tofacitinib (21.5 mg/kg，50% DMSO+10% PEG 400+40% water) 皮下注射給攜帶原位擴(kuò)散 MM.1S 異種移植物的 NSG 小鼠，每天一次，持續(xù)四周。結(jié)果: 小鼠存活率顯著提高，并且基于生物發(fā)光成像定量，腫瘤負(fù)荷顯著降低。[1]
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 3.12 mg/mL (9.99 mM), Sonication is recommended Ethanol : 0.76 mg/mL (2.43 mM), Sonication is recommended.
關(guān)鍵字	CP 690550 \| Janus kinase \| JAK \| Apoptosis \| Inhibitor \| Tofacitinib \| inhibit \| CP690550
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相關(guān)庫(kù)	經(jīng)典已知活性庫(kù) \| 抗癌上市藥物庫(kù) \| 已知活性化合物庫(kù) \| FDA 上市藥物庫(kù) \| TGF-β/Smad靶點(diǎn)化合物庫(kù) \| 藥物功能重定位化合物庫(kù) \| FDA 上市激酶抑制劑庫(kù) \| 酪氨酸激酶分子庫(kù) \| 抗癌臨床化合物庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字：托法替尼|||Tasocitinib|||CP-690550|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)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(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)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(guò)在中國(guó)市場(chǎng)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(guò)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(cè)資本	566.2651萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營(yíng)模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國(guó)（陶術(shù)生物）

VIP 12年

公司成立：12年
注冊(cè)資本：566.2651萬(wàn)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(yíng)產(chǎn)品：小分子抑制劑，藥物篩選化合物庫(kù)，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(chǎng)三路28號(hào)4樓

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