價格 | ¥153 | ¥236 | ¥388 |
包裝 | 5mg | 10mg | 25mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-09-29 |
中文名稱:化合物 GNF-5 | 英文名稱:GNF-5 |
CAS:778277-15-9 | 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: 99.98% | 產(chǎn)品類別: 抑制劑 |
貨號: T1803 |
名稱 | GNF-5 |
描述 | GNF-5 is a specific non-ATP competitive inhibitor of Bcr-Abl (IC50: 0.22±0.1 uM, Wild-type Abl). It is an analog of GNF-2 with improved pharmacokinetic properties. |
細(xì)胞實驗 | Ba/F3.p210 cells are obtained by transfecting the IL-3-dependent murine hematopoietic Ba/F3 cell line with a pEYK vector containing p210BCR-ABL and Bcr-Abl mutations. All cell lines are cultured with 5% CO2 at 37 °C in RPMI 1640 with 10% fetal bovine serum (FBS) and supplemented with 1% l-glutamine. Parental Ba/F3 cells are similarly cultured with 10% WEHI-conditioned medium as a source of IL-3. Transfected cell lines are cultured in media supplemented with 25 μg/mL zeocin. The 48 h cell proliferation studies are obtained using the CellTiter-Glo assay.(Only for Reference) |
激酶實驗 | Kinetic characterization of Abl inhibition: The ATP/NADH-coupled assay system in a 96-well format is used to determine the initial velocity of Abl tyrosine kinase catalyzed peptide phosphorylation. The reaction mixture contained 20 mM Tris-HCl, (pH 8.0), 50 mM NaCl, 10 mM MgCl2, 2 mM PEP [2-(Phosphonooxy)- 2-propenoic acid) and 20 μg Abl peptide substrate (EAIYAAPFAKKK), fixed or varied (to determine inhibitor kinetic parameters) concentration of inhibitor applied, 1/50 of the final reaction mixture volume of PK/LDH enzyme (pyruvate kinase/lactic dehydrogenase enzymes from rabbit muscle), 160 μM NADH, 0.16 μM Abl, and ATP added last to start the reaction. Absorbance data are collected every 20s at 340 nm using a SpectraMax M5 Microplate Reader. |
體外活性 | GNF-5(75 mg/kg)與尼羅替尼(50 mg/kg)聯(lián)用可使T315I Bcr-Abl BMT模型中總存活數(shù)提高.GNF-5(100 mg/kg)表現(xiàn)出對異種移植和骨髓移植模型中野生型和T315I Bcr-Abl依賴性增殖的療效. |
體內(nèi)活性 | GNF-5的抗增殖活性較強,可抑制wt-Bcr-Abl(EC50:430 nM)和E255K突變型(EC50:580 nM)Bcr-Abl細(xì)胞增殖。GNF-5與尼羅替尼或伊馬替尼聯(lián)用可抑制體外耐藥變異的出現(xiàn),且在抗Bcr-Abl T315I突變體的細(xì)胞試驗和生物化學(xué)中顯示了額外的抑制活性。 |
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 : 16 mg/mL (38.2 mM) DMSO : 16.67 mg/mL (39.84 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) |
關(guān)鍵字 | Inhibitor | Bcr-Abl | GNF-2 | pharmacokinetic | GNF-5 | cancer | Chronic myelogenous leukemia (CML) | GNF5 | inhibit |
相關(guān)產(chǎn)品 | Umifenovir hydrochloride | Imatinib | Chloroquine phosphate | Andrographolide | Hydroxychloroquine | EIDD-1931 | Chloroquine | Silymarin | Ritonavir | Nirmatrelvir | Favipiravir | Remdesivir |
相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 抗癌化合物庫 | 已知活性化合物庫 | 抗感染化合物庫 | 激酶抑制劑庫 | 細(xì)胞骨架化合物庫 | 抗病毒庫 | 酪氨酸激酶分子庫 | 表型篩選靶點鑒定庫 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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