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泊馬度胺,Pomalidomide

泊馬度胺|T2384|TargetMol

價(jià)格 429 644 831
包裝 10mg 50mg 100mg
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:泊馬度胺英文名稱:Pomalidomide
CAS:19171-19-8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: 98.8%產(chǎn)品類別: 抑制劑
貨號(hào): T2384
2024-12-02 泊馬度胺 Pomalidomide 10mg/429RMB;50mg/644RMB;100mg/831RMB 429 TargetMol 美國(guó) Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. 98.8% 抑制劑

Product Introduction

Bioactivity

名稱Pomalidomide
描述Pomalidomide (CC-4047) is an anti-angiogenic and immunomodulatory agent. Pomalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN) and is commonly used in the synthesis of PROTAC products.
細(xì)胞實(shí)驗(yàn)In vitro effects of either CC-5013 or CC-4047 as single agent or in combination with rituximab were evaluated by flow cytometric analysis. Lymphoma cell lines (1 × 10^6 cells) were exposed to either CC-5013 (5 μg/mL), CC-4047 (5 μg/mL), or vehicle control (DMRIE-C, 0.01%) alone or in combination with rituximab at a final concentration of 10 μg/mL. Following a period of incubation of 24 or 48 hours, apoptosis was assessed by staining-treated cells with FITC-labeled Annexin V and propidium iodine. All samples were analyzed by multicolor flow cytometric analysis using a fluorescence-activated cell sorter/FACStar Plus flow cytometer. Cells were scored as apoptotic if they were Annexin V–positive and propidium iodine–negative/positive (early and late apoptosis, respectively) [2].
激酶實(shí)驗(yàn)TNF-α inhibitory activity is measured in lipopolysacharide (LPS) stimulated PBMC. Pomalidomide is added to human PBMCs 1 hour prior to the addition of LPS (1 μg/mL) and incubation continued for an additional 18-20 hours. Supernatants are then harvested, and the concentration of TNF-α in the supernatants is determined by ELISA. The concentration of Pomalidomide that IC50 is calculated by nonlinear regression analysis [1].
動(dòng)物實(shí)驗(yàn)These studies were carried out using a disseminated lymphoma-bearing SCID mouse xenograft model. Raji cells were harvested from confluent cultures and only suspensions with >90% viable cells were used for animal inoculation. Subsequently, on day 0, SCID mice received 1 ×10^6 Raji cells via i.v. Untreated SCID mice inoculated by i.v. injection develop symptomatic central nervous system, pulmonary, and liver metastasis that result in death from massive tumor burden and central nervous system involvement after 17 to 21 days after inoculation. A second lymphoma mouse model was used to address the significance of NK cell expansion in the biological interactions observed between rituximab and IMiDs. The second mouse lymphoma xenograft consisted of SCID mice depleted of NK cells bearing Raji cells implanted via tail vein injection as described above [2].
體外活性方法: 多發(fā)性骨髓瘤細(xì)胞 RPMI8226 和 OPM2 用 Pomalidomide (0.01-50 μM) 處理 48 h,使用 MTT assay 檢測(cè)細(xì)胞活力。 結(jié)果: Pomalidomide 在 48 h 顯著降低 RPMI8226 和 OPM2 細(xì)胞的細(xì)胞活力,IC50 值分別為 8 μM 和 10 μM。[1] 方法: 多發(fā)性骨髓瘤細(xì)胞 H929、U266 和 MM.1s 用 Pomalidomide (0.05-1 μM) 和 ACY-241 (3 μM) 處理 4 天,使用 Flow cytometry 檢測(cè)細(xì)胞凋亡。 結(jié)果: 當(dāng)兩種藥物聯(lián)合治療時(shí),相對(duì)于任何一種單一藥物,細(xì)胞凋亡顯著增加。[2]
體內(nèi)活性方法: 為評(píng)估在腦缺血中的潛在價(jià)值,將 Pomalidomide (50 mg/kg,1% carboxy methyl cellulose) 腹腔注射給長(zhǎng)期過(guò)度表達(dá) TNF-α 表面活性蛋白 (SP)-C 啟動(dòng)子的轉(zhuǎn)基因小鼠 (SP-C/TNF-α 小鼠),每天一次,持續(xù) 21 天。 結(jié)果: Pomalidomide 顯著降低血清 TNF-α 和 IL-5水平。[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H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (182.99 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5.4 mg/mL (19.76 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Ligands for E3 Ligase | inhibit | Apoptosis | CC4047 | Molecular Glues | CC 4047 | Inhibitor | Pomalidomide | E3 ligase-recruiting Moiety
相關(guān)產(chǎn)品L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate
相關(guān)庫(kù)抗癌活性化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 抗衰老化合物庫(kù) | FDA 上市藥物庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌藥物庫(kù)
關(guān)鍵字: 泊馬度胺|||CC-4047|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
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