| 产品描述： | CHR-6494 is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 inhibits histone H3T3 phosphorylation. CHR-6494 can be used in the research of cancer |
| 靶点： |
haspin:2 nM (IC50) |
| 体内研究： |
CHR-6494 (50 mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumor and cuases no obvious body weight change in nude mice bearing HCT-116 human colorectal cancer cells. CHR-6494 (20 mg/kg; intraperitoneal injection for 15 consecutive days) inhibits the tumor volume and weight compared with the control group in nude mice bearing MDA-MB-231 xenograft tumors. CHR-6494 (20 mg/kg; intraperitoneal injection for 15 consecutive days) enhances the tumor volume and weight inhibition of MLN8237 (20 mg/kg; p.o.) in vivo |
| 参考文献： |
1. Huertas D, et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene. 2012 Mar 15;31(11):1408-18. 2. Han L, et al. Anti-Melanoma Activities of Haspin Inhibitor CHR-6494 Deployed as a Single Agent or in a Synergistic Combination with MEK Inhibitor. J Cancer. 2017 Aug 25;8(15):2933-2943. 3. Chen A, et al. CRISPR/Cas9 screening identifies a kinetochore-microtubule dependent mechanism for Aurora-A inhibitor resistance in breast cancer. Cancer Commun (Lond). 2021 Feb;41(2):121-139. |
| 溶解性： |
DMSO : 50 mg/mL (171.03 mM; Need ultrasonic) |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.421 ml |
17.103 ml |
34.207 ml |
| 5 mM |
0.684 ml |
3.421 ml |
6.841 ml |
| 10 mM |
0.342 ml |
1.71 ml |
3.421 ml |
| 50 mM |
0.068 ml |
0.342 ml |
0.684 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