舒尼替尼|T0374L

價(jià)格	￥543	￥1255	￥798
包裝	100mg	500mg	200mg

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(chēng):舒尼替尼	英文名稱(chēng):Sunitinib
CAS:557795-19-4	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: 99.67%	產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T0374L

Product Introduction

Bioactivity

名稱(chēng)	Sunitinib
描述	Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). Sunitinib has antitumor activity and can be used for the treatment of kidney cancer and gastrointestinal tumors.
細(xì)胞實(shí)驗(yàn)	Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3. (Only for Reference)
激酶實(shí)驗(yàn)	Biochemical Tyrosine Kinase Assays: IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferase fusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST.The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
體外活性	方法：FLT3-ITD 細(xì)胞系 MV4;11 和 FLT3-WT 細(xì)胞系 OC1-AML5 用 Sunitinib (0.001-10 μM) 處理 48 h，使用 Alamar blue assay 檢測(cè)細(xì)胞活力。結(jié)果：Sunitinib 以劑量依賴(lài)性方式顯著抑制 MV4;11和 OC1-AML5 細(xì)胞增殖，IC50 分別為 8 nM 和 14 nM。[1] 方法：胃腸道間質(zhì)瘤細(xì)胞 GIST-T1 用 Sunitinib (10-40 nM) 處理 48 h，使用 Western Blot 檢測(cè)靶點(diǎn)蛋白表達(dá)水平。結(jié)果：Sunitinib 以劑量依賴(lài)的方式抑制 c-KIT 的自磷酸化。Sunitinib 可有效阻斷 c-KIT 下游效應(yīng)子 Akt 和 ERK 的磷酸化，但不影響 STAT3 和 STAT5 的磷酸化形式。[2]
體內(nèi)活性	方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 Sunitinib (1-40 mg/kg in a citrate-buffered solution (pH 3.5)) 灌胃給藥給攜帶人白血病腫瘤 MV4;11 的 athymic nu/nu 小鼠，每天一次，至腫瘤消退。結(jié)果：Sunitinib 以 4 0和 20mg/kg/d 給藥時(shí)表現(xiàn)出劑量依賴(lài)性療效，并消退了已建立的大的皮下腫瘤。[1] 方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 Sunitinib (40-80 mg/kg in CMC) 灌胃給藥給注射乳腺癌細(xì)胞 MDA-MB-435/HAL 的 athymic nu/nu 小鼠，每天一次，持續(xù)二十一天。結(jié)果：Sunitinib 治療荷瘤小鼠后，血清 PYD 水平顯著降低，證實(shí)了骨溶解的體內(nèi)抑制作用。使用 BLI，Sunitinib 以 40mg/kg/天治療 21 天顯示出 64% 的骨腫瘤生長(zhǎng)抑制作用，以 80mg/kg/天顯示出 89% 的抑制作用。[3]
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	DMSO : 25 mg/mL (62.74 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1.25 mg/mL (3.14 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
關(guān)鍵字	Sunitinib \| PDGFR \| Inositol requiring enzyme 1 \| IRE1 \| Platelet-derived growth factor receptor \| Autophagy \| Mitophagy \| Vascular endothelial growth factor receptor \| inhibit \| Inhibitor \| SU11248 \| VEGFR \| SU-11248 \| Apoptosis \| Mitochondrial Autophagy
相關(guān)產(chǎn)品	Guanidine hydrochloride \| Naringin \| Hydroxychloroquine \| Stavudine \| L-Ascorbic acid \| Paeonol \| Sodium 4-phenylbutyrate
相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 抗癌活性化合物庫(kù) \| EMA 上市藥物庫(kù) \| 激酶抑制劑庫(kù) \| FDA 上市藥物庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 酪氨酸激酶分子庫(kù) \| 藥物功能重定位化合物庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字：蘇尼替尼|||舒尼替尼|||SU 11248|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(zhuān)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(xiāo)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(mǎn)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(lèi)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)

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公司成立：12年
注冊(cè)資本：566.2651萬(wàn)人民幣
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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
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