Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GNF-5是 Bcr-Abl 的特异性非 ATP 竞争性抑制剂,IC50为0.22uM。它是 GNF-2 的类似物,具有改进的药代动力学特性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 257 | 现货 | ||
10 mg | ¥ 393 | 现货 | ||
25 mg | ¥ 647 | 现货 | ||
50 mg | ¥ 987 | 现货 | ||
100 mg | ¥ 1,730 | 现货 | ||
200 mg | ¥ 2,580 | 现货 | ||
500 mg | ¥ 4,270 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 262 | 现货 |
产品描述 | 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. |
靶点活性 | Bcr-Abl:0.22±0.1 μM |
体外活性 | GNF-5(75 mg/kg)与尼罗替尼(50 mg/kg)联用可使T315I Bcr-Abl BMT模型中总存活数提高.GNF-5(100 mg/kg)表现出对异种移植和骨髓移植模型中野生型和T315I Bcr-Abl依赖性增殖的疗效. |
体内活性 | GNF-5的抗增殖活性较强,可抑制wt-Bcr-Abl(EC50:430 nM)和E255K突变型(EC50:580 nM)Bcr-Abl细胞增殖。GNF-5与尼罗替尼或伊马替尼联用可抑制体外耐药变异的出现,且在抗Bcr-Abl T315I突变体的细胞试验和生物化学中显示了额外的抑制活性。 |
激酶实验 | 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. |
细胞实验 | 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) |
别名 | GNF 5 |
分子量 | 418.37 |
分子式 | C20H17F3N4O3 |
CAS No. | 778277-15-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 16 mg/mL (38.2 mM)
DMSO: 77 mg/mL (184 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.3902 mL | 11.9511 mL | 23.9023 mL | 59.7557 mL |
5 mM | 0.478 mL | 2.3902 mL | 4.7805 mL | 11.9511 mL | |
10 mM | 0.239 mL | 1.1951 mL | 2.3902 mL | 5.9756 mL | |
20 mM | 0.1195 mL | 0.5976 mL | 1.1951 mL | 2.9878 mL | |
DMSO | 50 mM | 0.0478 mL | 0.239 mL | 0.478 mL | 1.1951 mL |
100 mM | 0.0239 mL | 0.1195 mL | 0.239 mL | 0.5976 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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