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伊布替尼,Ibrutinib

伊布替尼|T1835主打

價(jià)格 ￥488 ￥788 ￥1995
包裝 5mg 10mg 50mg
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:伊布替尼英文名稱:Ibrutinib
CAS:936563-96-1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: 99.79%產(chǎn)品類別: 抑制劑
貨號(hào): T1835
2024-12-02 伊布替尼 Ibrutinib 5mg/488RMB;10mg/788RMB;50mg/1995RMB 488 TargetMol 美國(guó) Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. 99.79% 抑制劑

Product Introduction

Bioactivity

名稱Ibrutinib
描述Ibrutinib (PCI-32765) is a Bruton's tyrosine kinase (BTK) inhibitor (IC50=0.5 nM) with irreversible and selective properties. Ibrutinib blocks BTK to inhibit the proliferation and survival of B cells, and possesses antitumor activity, which can be used for the treatment of chronic lymphocytic leukemia, among others.
細(xì)胞實(shí)驗(yàn)CD20+ B and CD3+ T cells were purified by negative selection (RosetteSep, >90% purity) from buffy coat PBMCs and viably frozen in 10% DMSO. Cells were thawed at 37 °C and maintained in growth media (RPMI media containing 10% FCS). B cells were stimulated with goat anti-human IgM F(ab′)2 (10 μg/mL) and T cells were stimulated with anti-CD3/CD28 coated beads at a 1:1 bead/cell ratio. Cells were stained with PE-CD69 and analyzed by flow cytometry, gating on viable lymphocytes. PCI-32765 at concentrations lower than 10 μM did not decrease B- or T-cell viability during the course of the experiment, although PCI-32765 did block the modest survival benefit of anti-IgM stimulation in B cells. For washout experiments, cells were rinsed three times in 10 volumes of growth media, a protocol that was confirmed to completely wash away inhibition of BCR signaling by PCI-29732, a reversible Btk inhibitor [1].
激酶實(shí)驗(yàn)In vitro kinase IC50s were measured using 33P filtration binding assay after 1 h incubation of kinase, 33P-ATP, inhibitor, and substrate [0.2 mg/mL poly(EY)(4:1]. Assays were performed at Reaction Biology [1].
動(dòng)物實(shí)驗(yàn)ale DBA/1 mice were immunized with type II collagen plus Freund adjuvant and boosted 21 d later. On a rolling basis, as significant swelling appeared in at least one paw, mice were enrolled and randomized. PCI-32765 or dexamethasone (0.2 mg/kg) was administered orally once per day for 11 d. Arthritis scores (0–5) were assigned to the mice based on the degree and extent of paw swelling. Mouse anti-type II collagen antibody and total IgG levels were measured by ELISA. Female MRL/MpJ-Faslpr mice received PCI-32765 by oral gavage once per day from week 8 through week 20. Proteinuria was monitored weekly. At week 20, serum was collected and analyzed for BUN and mouse anti-dsDNA antibody levels. Kidney histology was scored according to established criteria (26). No drug-induced weight loss was observed at any of the dose levels tested. These studies were carried out at Boulder Biopath according to approved animal care protocols. Results are presented as the mean ± SEM. Statistical significance between groups were evaluated with repeated measures one-way ANOVA or one-way ANOVA using GraphPad Prism with Tukey or Bonferroni multicomparison posttest [1].
體外活性方法：人 B 細(xì)胞淋巴瘤細(xì)胞 DOHH2 用 Ibrutinib (0.00064-2 μM) 孵育 1 h，再用 anti-IgG F(ab′)2 (30 μg/mL) 刺激 2 min，使用 Western Blot 檢測(cè)靶點(diǎn)蛋白表達(dá)水平。 結(jié)果：Ibrutinib 抑制 Btk 的自體磷酸化 (IC50=11 nM)，Btk 的生理底物 PLCγ 的磷酸化 (IC50=29 nM)，和進(jìn)一步的下游激酶 ERK 的磷酸化 (IC50=13 nM)。[1] 方法：原代人類B淋巴細(xì)胞用 Ibrutinib (1-1000 nM) 處理 30 min，然后用 anti-IgM F(ab')2 (10 μg/mL)、anti-CD3/CD28 (5 μg/mL) 或 PMA (0.5 μg/mL) 刺激細(xì)胞 72 h，使用 Cell Titer Glo reagent 檢測(cè)細(xì)胞增殖。 結(jié)果：Ibrutinib 劑量依賴性地抑制抗 IgM 刺激的 B 淋巴細(xì)胞增殖 (IC50=8 nM)，但不抑制 PMA 刺激的增殖，PMA 激活PKC途徑。[2]
體內(nèi)活性方法：為檢測(cè)體內(nèi)抗炎活性，將 Ibrutinib (3.125-50 ?mg/kg) 灌胃給藥給關(guān)節(jié)炎 DBA/1 小鼠，每天一次，持續(xù)十一天。 結(jié)果：在所有劑量下治療的小鼠中觀察到臨床關(guān)節(jié)炎評(píng)分的顯著抑制。在分別以 3.125 和 12.5 mg/kg/天 的劑量治療 9 至 11 天后，疾病的臨床癥狀出現(xiàn)部分和幾乎完全消除。與體內(nèi)抑制 B 細(xì)胞活化一致，抗膠原自身抗體的產(chǎn)生顯著減少，總 IgG 水平適度降低。[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10% DMSO+40% PEG300+5% Tween 80+45% Saline : 8.2 mg/mL (18.62 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.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 45 mg/mL (102.16 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
關(guān)鍵字inhibit | PCI 32765 | Ligands for Target Protein for PROTAC | Target Protein-binding Moiety | PCI32765 | Inhibitor | Btk | Ibrutinib | Bruton tyrosine kinase
相關(guān)產(chǎn)品Pelitinib | Deucravacitinib | Gefitinib | Vemurafenib | Ruxolitinib | (+)-JQ-1 | Staurosporine | Nintedanib | Dasatinib | Baricitinib | GSK 3 Inhibitor IX | Delgocitinib
相關(guān)庫抗癌上市藥物庫 | 抗癌活性化合物庫 | 經(jīng)典已知活性庫 | EMA 上市藥物庫 | FDA 上市藥物庫 | 酪氨酸激酶分子庫 | 抗癌臨床化合物庫
關(guān)鍵字： 依魯替尼|||伊布替尼|||PCI-32765|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，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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