手机验证
Bosutinib,别名: SKI-606
380843-75-4
10
研卉生物
25mg
产品描述 |
Bosutinib is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases. |
靶点活性 |
Abl,1nM c-Src,1.2nM MAPK, |
体外活性 |
Bosutinib 能够明显抑制Bcr-Abl阳性白血病细胞系KU812(IC50=5 nM), K562(IC50=20 nM), 和MEG-01(IC50=20 nM)。Bosutinib作用于Src (IC50=1.2 nM),且有效抑制Src依赖的细胞增殖(IC50=100 nM)。Bosutinib可对乳腺癌细胞运动和入侵有降低(IC50=250 nM),提高细胞间粘附和β-连环蛋白的膜定位。 |
体内活性 |
在携带Src-转化纤维移植瘤和HT29移植瘤的裸鼠中,每天用Bosutinib(60 mg/kg)处理,有效抑制肿瘤。在携带Colo205移植瘤的裸鼠中,每天两次用Bosutinib(75 mg/kg)处理,可抑制肿瘤生长,提高剂量后不会有更高效果。小鼠口服Bosutinib100 mg/kg剂量处理可根除大的肿瘤,按150 mg/kg剂量处理可除去肿瘤,且没有毒性。 |
激酶实验 |
The Src and Abl kinase assays: The Src kinase activity is measured in an ELISA format. Src (3 units/reaction), reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.5 mM Na3VO4) and cdc2 substrate peptide are added to various concentration of Bosutinib and incubated at 30 °C for 10 minutes. The reaction is started by the addition of ATP to a final concentration of 100 μM, incubated at 30 °C for 1 hour and stopped by addition of EDTA. Instructions from the manufacturer are followed for subsequent steps. The Abl kinase assay is performed in a DELFIA solid phase europium-based detection assay format. Biotinylated peptide (2 μM) is bound to streptavidin-coated microtitration plates for 1.5 hours in 1 mg/mL ovalbumin in PBS. The plates are washed for 1 hour with PBS/0.1% Tween 80, followed by a PBS wash. The kinase reaction is incubated for 1 hour at 30°C. Abl kinase (10 units) is mixed with 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, 80 μM EGTA, 100 μM ATP, 0.5 mM Na3VO4, 1% DMSO, 1 mM HEPES (pH 7.0), 200 μg/mL ovalbumin and various concentration of Bosutinib. The reaction is stopped with EDTA at a final concentration of 50 mM. The reaction is monitored with Eu-labeled phosphotyrosine antibody and DELFIA enhancement solution. |
细胞实验 |
Cells are exposed to various concentrations of Bosutinib for 72 hours. Anchorage-independent proliferation of Abl-MLV-transformed fibroblasts is measured in 96-well ultra-low binding plates treated with Sigmacote to block residual cell attachment. Cell proliferation is measured with MTS or Cell-Glo. For the determination of cell cycle or cell death, cells are prepared for FACS analysis in the CycleTest Plus DNA reagent kit and analyzed on a fluorescence-activated cell sorter flow cytometer. (Only for Reference) 细胞系: Abl-MLV, Rat 2, KU812, K562, and MEG-01 cells |
动物实验 |
动物模型:Nude femice injected with K562 cells |
化学信息
分子量 |
530.45 |
分子式 |
C26H29Cl2N5O3 |
CAS |
380843-75-4 |
溶解度 |
DMSO: 53.1 mg/mL (100 mM) Ethanol: 13.3 mg/mL (25 mM) ( < 1 mg/ml refers to the product slightly soluble or insoluble ) |
储存条件 |
store at -80°C |
备注 |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
配制溶液
1 mg | 5 mg | 10 mg | |
1 mM | 1.885 ml | 9.426 ml | 18.852 ml |
5 mM | 0.377 ml | 1.885 ml | 3.77 ml |
10 mM | 0.189 ml | 0.943 ml | 1.885 ml |
50 mM | 0.038 ml | 0.189 ml | 0.377 ml |
参考文献
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