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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。
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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 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 153 | 现货 | |
10 mg | ¥ 236 | 现货 | |
25 mg | ¥ 388 | 现货 | |
50 mg | ¥ 592 | 现货 | |
100 mg | ¥ 1,030 | 现货 | |
200 mg | ¥ 1,530 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 157 | 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 |
Smiles | N(C1=CC(=NC=N1)C2=CC(C(NCCO)=O)=CC=C2)C3=CC=C(OC(F)(F)F)C=C3 |
密度 | 1.385 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | Ethanol: 16 mg/mL (38.2 mM) DMSO: 16.67 mg/mL (39.84 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||
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