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 |
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 |
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) |
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