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• 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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *