卡非佐米|T1795

價格	￥526	￥858	￥1510
包裝	5mg	10mg	25mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:卡非佐米	英文名稱:Carfilzomib
CAS:868540-17-4	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: 99.84%	產(chǎn)品類別: 抑制劑
貨號: T1795

Product Introduction

Bioactivity

名稱	Carfilzomib
描述	Carfilzomib (PR-171) is a proteasome inhibitor that irreversibly binds to the chymotrypsin of the 20S proteasome. Carfilzomib has antitumor activity and may be used to treat multiple myeloma.
細(xì)胞實驗	WST-1 is used to determine the effects of proteasome inhibitor Carfilzomib on cell proliferation. The inhibition of proliferation is calculated in relation to parallel control cells that receives vehicle alone. A linear spline function is used to interpolate the median inhibitory concentration (IC50) using XLfit 4 software. The degree of resistance (DOR) is calculated using the formula: DOR = IC50(resistant cells)/IC50(sensitive cells). ANBL-6 cells pulsed with 100 nM carfilzomib are washed and suspended in PBS containing 5 μg/mL of JC-1, which exhibits potential-dependent accumulation in mitochondria. Analysis of the mitochondrial membrane potential-dependent color shift from 525 to 590 nm is carried out on a FacScan, and the data are analyzed with CellQuest software.(Only for Reference)
激酶實驗	Enzyme-linked immunosorbent assay for subunit profiling of carfilzomib: ANBL-6 cells (2 × 106/well) are plated in 96-well plates and treated with Carfilzomib doses from 0.001 to 10 μM for 1 hour. Cells are then lysed (20 mM Tris-HCl, 0.5 mM EDTA), and cleared lysates are transferred to polymerase chain reaction (PCR) plates. A standard curve is generated using untreated ANBL-6 cell lysates starting at a concentration of 6 μg protein/μL. The active site probe [biotin-(CH2)4-Leu-Leu-Leu-epoxyketone; 20 μM] is added and incubated at room temperature for 1 hour. Cell lysates are then denatured by adding 1% sodium dodecyl sulfate (SDS) and heating to 100°C, followed by mixing with 20 μL per well streptavidin-sepharose high-performance beads in a 96-well multiscreen DV plate and incubated for 1 hour. These beads are then washed with enzyme-linked immunosorbent assay (ELISA) buffer (PBS, 1% bovine serum albumin, and 0.1% Tween-20), and incubated overnight at 4°C on a plate shaker with antibodies to proteasome subunits. Antibodies used included mouse monoclonal anti-β1, anti-β2, anti-β1i, and anti-β5i, goat polyclonal anti-β2i, and rabbit polyclonal anti-β5 (affinity-purified antiserum against KLH-CWIRVSSDNVADLHDKYS peptide). The beads are washed and incubated for 2 hours with horseradish peroxidase-conjugated secondary goat antirabbit, goat antimouse or rabbit antigoat antibodies. After washing, the beads are developed using the supersignal ELISA picochemiluminescence substrate. Luminescent detection is performed. Raw luminescence is converted to μg/mL by comparison with the standard curve and expressed as the % inhibition relative to vehicle control. Curve fits are generated using the following nonsigmoidal dose-response equation: Y = Bottom + (Top-Bottom)/(1 + 10?((LogEC50 ? X) × HillSlope)), where X is the logarithm of concentration, Y is the % inhibition, and EC50 is the dose showing 50% effect.
體外活性	方法：骨髓瘤細(xì)胞系 RPMI 8226 和 ANBL-6 用 Carfilzomib (0-25 nM) 處理 24 h，使用 WST-1 assay 檢測細(xì)胞活力。結(jié)果：Carfilzomib 處理劑量依賴性降低 RPMI 8226 和 ANBL-6 細(xì)胞的細(xì)胞活力，IC50 均小于 5 nM。[1] 方法：B 細(xì)胞淋巴瘤細(xì)胞系 Raji、Raji-2R 和 Raji-4RH 用 Carfilzomib (1-10 nM) 處理 24-72 h，使用 Flow Cytometry 分析細(xì)胞凋亡情況。結(jié)果：Carfilzomib 誘導(dǎo) B 細(xì)胞淋巴瘤細(xì)胞系發(fā)生凋亡，細(xì)胞凋亡的程度是與時間相關(guān)的。[2]
體內(nèi)活性	方法：為檢測體內(nèi)抗腫瘤活性，將 Carfilzomib (5 mg/kg，10% captisol) 靜脈注射給攜帶套細(xì)胞淋巴瘤 (MCL) Mino 的 SCID 小鼠，每周兩次，持續(xù)五周。結(jié)果：Carfilzomib 幾乎消除了腫瘤生長，并顯著延長了荷瘤小鼠的生存時間。[3] 方法：為檢測體內(nèi)抗腫瘤活性，將 Carfilzomib (6 mg/kg，10% captisol) 腹腔注射給轉(zhuǎn)移性無定形甲狀腺腫瘤 (ATC) 小鼠模型，每周三次，持續(xù)三周。結(jié)果：Carfilzomib 治療患有已確定的廣泛轉(zhuǎn)移性疾病的小鼠顯著提高了它們的存活率，但沒有顯著毒性。[4]
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 55 mg/mL (76.4 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5.5 mg/mL (7.64 mM), Suspension. 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.
關(guān)鍵字	PR 171 \| Inhibitor \| Proteasome \| Apoptosis \| Carfilzomib \| inhibit \| Autophagy \| PR171
相關(guān)產(chǎn)品	Guanidine hydrochloride \| Naringin \| Valproic Acid \| L-Glutamic acid \| Gefitinib \| Hydroxychloroquine \| Dextran sulfate sodium salt (MW 4500-5500) \| Stavudine \| Tributyrin \| L-Ascorbic acid \| Paeonol \| Sodium 4-phenylbutyrate

關(guān)鍵字：卡非佐米|||PR-171|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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