产品描述: CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively. |
靶点:
Aurora A:15 nM (IC50);Aurora B:25 nM (IC50);Aurora C:19 nM (IC50);Apoptosis;AuroraKinase;Autophagy |
体内研究:
CCT 137690 slows the growth of the SW620 xenografts with no observed toxicity. CCT 137690 significantly inhibits tumour growth in a transgenic mouse model of neuroblastoma (TH-MYCN) that overexpresses MYCN protein and is predisposed to spontaneous neuroblastoma formation |
参考文献:
1. Bavetsias V, et al. Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. J Med Chem. 2010 Jul 22;53(14):5213-28. 2. Faisal A, et al. The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Mol Cancer Ther. 2011 Nov;10(11):2115-23. |
溶解性:
Soluble in DMSO |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
1.813 ml |
9.067 ml |
18.133 ml |
5 mM |
0.363 ml |
1.813 ml |
3.627 ml |
10 mM |
0.181 ml |
0.907 ml |
1.813 ml |
50 mM |
0.036 ml |
0.181 ml |
0.363 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。 |