| 产品描述: | JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2. |
| 靶点: |
Apoptosis;Aurora Kinase;CDK;Apoptosis;CDK;AuroraKinase |
| 体内研究: |
JNJ-7706621在抑制正常细胞类型(包括MRC-5,HASMC,HUVEC和HMVEC)的生长方面具有几倍的效力,IC50为3.67-5.42 μM。JNJ-7706621对CDK1和2具有高度有效性,IC50为3-9 nM。JNJ-7706621显示对包括HeLa,HCT-116,SK-OV-3,PC3,DU145,A375,MDA-MB-231,MES-SA和MES-SA/Dx5在内的一组人类癌细胞类型的抑制作用 ,IC50为112-514 nM,独立于p53,成视网膜细胞瘤或P-糖蛋白状态。JNJ-7706621也抑制CDK3,4和6,IC50为58-253 nM。JNJ-7706621抑制Aurora-A和B,IC50分别为11和15 nM。JNJ-7706621也抑制VEGF-R2,FGF-R2和GSK3β,IC50为154-254 nM。在HeLa或U937细胞中,JNJ-7706621(0.5-3 μM)延迟从G1期中退出,使细胞停滞在G2-M期,诱导核内复制,激活凋亡并减少集落形成 |
| 细胞实验: |
Cell lines: HeLa,HCT-116,A375,SK-OV-3,MDA-MB-231 and PC-3 cells. Concentrations: 1 nM - 10 μM,dissolved in DMSO. Method: Measuring incorporation of 14C-labelled thymidine into newly synthesized DNA within the cells to determine the ability of JNJ-7706621 to inhibit the proliferation of cell growth.Cells are trypsinized and counted and 3-8 ×103 cells are added to each well of a 96-well CytoStar tissue culture treated scintillating microplate in 100 μL complete medium in a volume.Cells are incubated for 24 hours at 37 °C in an atmosphere containing 5% CO2.Next,1 μL JNJ-7706621 is added to the wells of the plate.Cells are incubated for another 24 hours.Methyl 14C-thymidine 56 mCi/mmol is diluted in complete medium and 0.2 μCi/well is added to each well of the CytoStar plate in a volume of 20 μL.The plate is incubated for 24 hours at 37 °C in JNJ-7706621 with 14C-thymidine.The contents of the plate are discarded and the plate is washed twice with 200 μL PBS.200 μL of PBS is added to each well.The top of the plate |
| 动物实验: |
Animal Models: Mouse xenograft model of A375 cellsFormulation & . Dosages: Dissolved in 0.5% methylcellulose containing 0.1% polysorbate 80 in sterile water.100 or 125 mg/kg. Administration: Orally or by intraperitoneal injection |
| 参考文献: |
1.Seamon JA, et al. Mol Cancer Ther, 2006, 5(10), 2459-2467. 2.Lin R, et al. J Med Chem, 2005, 48(13), 4208-4211. 3.Emanuel S, et al. Cancer Res, 2005, 65(19), 9038-9046. |
| 溶解性: |
Ethanol:<1 mg/mL DMSO:73 mg/mL (185.1 mM) H2O:<1 mg/mL |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.536 ml |
12.679 ml |
25.358 ml |
| 5 mM |
0.507 ml |
2.536 ml |
5.072 ml |
| 10 mM |
0.254 ml |
1.268 ml |
2.536 ml |
| 50 mM |
0.051 ml |
0.254 ml |
0.507 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |