Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GNF-7 是一种多重激酶抑制剂。它对ACK1和GCK 具有抑制活性,IC50分别为 25 nM 和 8 nM。它是一种 Bcr-Abl 的抑制剂,对 Bcr-AblWT 和 Bcr-AblT315I 作用的IC50值分别为 133 nM 和 61 nM。它可用于研究血液恶性肿瘤。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 369 | 现货 | ||
2 mg | ¥ 528 | 现货 | ||
5 mg | ¥ 897 | 现货 | ||
10 mg | ¥ 1,490 | 现货 | ||
25 mg | ¥ 2,890 | 现货 | ||
50 mg | ¥ 4,330 | 现货 | ||
100 mg | ¥ 6,180 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 997 | 现货 |
产品描述 | GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively. |
靶点活性 | BCR-ABL (WT):133 nM, BCR-ABL:61 nM |
体外活性 | GNF-7 shows potent antiproliferative activity against wild-type and mutant Bcr-Abl Ba/F3 cells with IC50 less than 11 nM. In human colon cancer cells (Colo205 and SW620), GNF-7 also displays excellent growth inhibitory activity with IC50 of 5 nM and 1 nM, respectively. [1] GNF-7, potently and selectively inhibits NRAS-dependent acute myelogenous leukemia and acute lymphoblastic leukemia cells through combined inhibition of ACK1/AKT and GCK. [2] |
体内活性 | GNF-7 exhibits excellent pharmacokinetic parameters in mice. In a bioluminescent xenograft mouse model using a transformed T315I-Bcr-Abl-Ba/F3 cell line, GNF-7 (10 mg/kg, p.o.) effectively inhibits tumor growth. [1] In NSG mice bearing human mutant NRAS-expressing MOLT-3-luc+ tumors, GNF-7 (15 mg/kg, p.o.) significantly decreases disease burden, prolongs overall survival, and causes strong suppression of phospho-AKT and phospho-RPS6. [2] |
激酶实验 | For kinase assays, purified CDC5L(295-795)-His6 is mixed with [γ-32P]ATP, COS-7 cell extract, and incubated in 100 μL 20 mM HEPES, pH 7.5, 50 mM NaCl, 2 mM MnCl2, 10 mM MgCl2, 0.5% NP-40, 0.5 mM PMSF, 5 mM benzamidine hydrochloride, 5 mM NaF, 1 mM NaVO3 and the specific inhibitor at 30°C for 10 minutes. Cell extract as a source of kinase activity is prepared from subconfluent, serum-stimulated COS-7 cells lysed in 20 mM HEPES-NaOH, pH 7.5, 50 mM NaCl, 1% Triton X-100, 10% glycerol, protease and phosphotase inhibitors. Phosphorylated proteins are separated by electrophoresis in 15% polyacrylamide-SDS gels. Specific inhibitors included 20 μM staurosporine, 10 μM genistein, 1 μM CVT-313, 10 μM Rp-MB-cAMPS and 50 μM PD98059[1]. |
别名 | GNF7 |
分子量 | 547.53 |
分子式 | C28H24F3N7O2 |
CAS No. | 839706-07-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 16 mg/mL (29.2 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 |
DMSO | 1 mM | 1.8264 mL | 9.1319 mL | 18.2638 mL | 45.6596 mL |
5 mM | 0.3653 mL | 1.8264 mL | 3.6528 mL | 9.1319 mL | |
10 mM | 0.1826 mL | 0.9132 mL | 1.8264 mL | 4.566 mL | |
20 mM | 0.0913 mL | 0.4566 mL | 0.9132 mL | 2.283 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。
GNF-7 839706-07-9 Angiogenesis Cytoskeletal Signaling Neuroscience Tyrosine Kinase/Adaptors Bcr-Abl ACK AChR GNF 7 inhibit Inhibitor leukemia T315I GNF7 mutation chronic CML Ack1 myelogenous TNK2 Activated Cdc42 kinase 1 AML inhibitor