| 产品描述： | Tizaterkib (AZD0364) is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM. |
| 靶点： |
ERK2:0.6 nM (IC50);ERK |
| 体外研究： |
Tizaterkib is measured in the ERK2 mass spectrometry and A375 phospho-p90RSK assays with IC50s of 0.6 nM and 5.7 nM, respectively. Tizaterkib can inhibit the growth of a panel of cancer cell lines (A549, H2122, H2009, and Calu6 cell lines) with KRAS mutations as a monotherapy and this effect is synergistically enhanced by treatment with Selumetinib |
| 体内研究： |
Tumor growth inhibition by Tizaterkib ethanesulfonic acid (Example 18a) in combination with MEK inhibitor Selumetinib is measured. Studies are performed in the A549 xenograft model. Selumetinib is dosed twice daily (BiD) 8 hours apart and Tizaterkib ethanesulfonic acid is dosed once daily (QD) 4 hours after the first Selumetinib dose. Both compounds are dosed continuously for 3 weeks. Both vehicles are dosed in the vehicle group. Both Selumetinib and Tizaterkib ethanesulfonic acid reduce tumor growth relative to vehicle only control. The combination of Selumetinib and Tizaterkib ethanesulfonic acid results in a reduction in tumor growth |
| 参考文献： |
1. WARD, Richard, Andrew, et al. DIHYDROIMIDAZOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER. WO2017080979A1. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20°C |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.022 ml |
10.111 ml |
20.222 ml |
| 5 mM |
0.404 ml |
2.022 ml |
4.044 ml |
| 10 mM |
0.202 ml |
1.011 ml |
2.022 ml |
| 50 mM |
0.04 ml |
0.202 ml |
0.404 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京