现货,JNJ-7706621, CAS号:443797-96-4,美国进口,细胞周期(Cell Cycle / Checkpoint) , CDK , CDK 抑制剂 ,selleck,目录号S1249

信号转导通路: 细胞周期(Cell Cycle / Checkpoint) >> CDK >> CDK 抑制剂和化合物 >> JNJ-7706621http://www.selleck.cn/jnj-7706621-S1249.html

技术数据:

分子量(MW): 394.36

化学式:

C15H12F2N6O3S

 

溶解度: DMSO ≥79mg/mL Water <1mg/mL Ethanol ≥3mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 443797-96-4

生物活性

 

 

JNJ-7706621 is a dual cyclin-dependent kinases and aurora kinases inhibitor with IC50 of 9 and 11 nM for CDK1/Cyclin B and aurora-A, respectively. JNJ-7706621 blocked proliferation of cancer cells regardless of their p53, retinoblastoma or P-glycoprotein status and induced cell death by activating apoptosis. JNJ-7706621 was about 10 fold less effective at inhibiting proliferation of normal cells. Flow cytometric analysis of DNA content in human tumor cells showed that JNJ-7706621 delayed progression through G1 and arrested the cell cycle at the G2/M phase. JNJ-7706621 also decreased CDK1 kinase activity, altered CDK1 phosphorylation status and blocked signaling to downstream substrates of CDKs. Additional cellular effects including endoreduplication and reduced histone H3 phosphorylation were also observed due to inhibition of Aurora kinase. JNJ-7706621 demonstrated significant inhibition of tumor growth in a variety of tumor types in nude mice xenograft models. In vitro cell proliferation assays IC50 (μM): HeLa (IC50=0.286), HCT-116 (IC50=0.189), PC3 (IC50=0.112). JNJ-7706621 is not affected by P-glycoprotein. [1][2][3]

 

 

 

参考文献

The In vitro and In vivo Effects of JNJ-7706621: A Dual Inhibitor of Cyclin-Dependent Kinases and Aurora Kinases Catherine A. Rugg, Robert H. Gruninger, et al. Cancer Res 2005;65:9038-9046

Preclinical profile of JNJ-7706621: A dual cyclin dependent kinase and aurora kinase inhibitor Stuart L. Emanuel,et al. Proc Amer Assoc Cancer Res. 2006;47

Evaluation of the CDK inhibitor JNJ-7706621 as a targeted antitumor agent Stuart L. Emanuel,et al. Proc Amer Assoc Cancer Res. 2004;45

 

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