化合物GNF-5 T1803

Product Introduction
Bioactivity


英文名: GNF-5

描述: 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。

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)

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.

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。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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)


关键字: Inhibitor | Bcr-Abl | GNF-2 | pharmacokinetic | GNF-5 | cancer | Chronic myelogenous leukemia (CML) | GNF5 | inhibit

相关产品: Z-FA-FMK | Bemnifosbuvir hemisulfate | D1N52 | WU-04 | Scutellarein | ML188 | E07 aptamer | Sivelestat | SARS-CoV-2-IN-59 | Zevotrelvir

相关库: Anti-Cancer Compound Library | Angiogenesis related Compound Library | Fluorochemical Library | Kinase Inhibitor Library | Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library | Tyrosine Kinase Inhibitor Library | Target-Focused Phenotypic Screening Library | Anti-Viral Compound Library | Bioactive Compound Library

化合物GNF-5 T1803信息由TargetMol中国为您提供，如您想了解更多关于化合物GNF-5 T1803报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途