| 产品描述： | UNC2025 is a potent, ATP-competitive and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia |
| 靶点： |
IC50: 0.74 nM (Mer); 0.8 nM (Flt3);FLT; TAMReceptor |
| 体内研究： |
UNC2025 (intravenous injection or oral adminstration; 3 mg/kg) exhibits an excellent PK properties: low clearance (9.2 mL/min kg), longer half-life (3.8 h), and high oral exposure (100%), it shows Tmax, Cmax, and AUClast 0.50 hour, 1.6 μM, and 9.2 h μM, respectively. UNC2025 (orally adminstration; 50 or 75 mg/kg; 34 and 70 days) mediates a statistically significant dose-dependent reduction in tumor burden relative to vehicle. mediates dose-dependent increases in median survival from 26 days after initiation of treatment in vehicle-treated mice, to 34 and 70 days in mice treated with 50 or 75 mg/kg UNC2025, respectively. |
| 参考文献： |
1. Zhang W, et al. UNC2025, a Potent and Orally Bioavailable MER/FLT3 Dual Inhibitor. J Med Chem. 2014 Aug 28;57(16):7031-41. 2. DeRyckere D, et al. UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with CL14377 in Leukemia Models.Clin Cancer Res. 2017 Mar 15;23(6):1481-1492. |
| 溶解性： |
DMSO : 100 mg/mL (209.79 mM; Need ultrasonic) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.098 ml |
10.49 ml |
20.979 ml |
| 5 mM |
0.42 ml |
2.098 ml |
4.196 ml |
| 10 mM |
0.21 ml |
1.049 ml |
2.098 ml |
| 50 mM |
0.042 ml |
0.21 ml |
0.42 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