| 產(chǎn)品描述： | UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC50s of <10 nM and 45 nM, repectively. |
| 靶點(diǎn)： |
IC50: <10 nM (EZH2), 45 nM (EZH1);HistoneMethyltransferase;?Autophagy |
| 體內(nèi)研究： |
A single intraperitoneal (IP) injection of UNC1999 at 15, 50, or 150 mg/kg achieved high Cmax?(9,700-11,800 nM) and exhibited dose linearity in male Swiss albino mice. Both the 150 and 50 mg/kg IP doses resulted in the plasma concentrations of UNC1999 above its cellular IC50?over the entire 24 h period while the 15 mg/kg IP dose led to the plasma concentrations of UNC1999 above its cellular IC50?for approximately 12 h. We next examined whether UNC1999 is orally bioavailable and are pleased to find that a single 50 mg/kg oral dose of UNC1999 achieved high Cmax?(4,700 nM) and good exposure levels in male Swiss albino mice. The plasma concentrations of UNC1999 are maintained above its cellular IC50?for approximately 20 h following this single oral dose. It is worth noting that all doses including the 150 mg/kg IP dose are well tolerated by all test mice, and no adverse effects are observed |
| 參考文獻(xiàn)： |
1. Konze KD, et al. An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34. |
| 溶解性： |
DMSO : 100 mg/mL (175.52 mM; Need ultrasonic) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.755 ml |
8.776 ml |
17.552 ml |
| 5 mM |
0.351 ml |
1.755 ml |
3.51 ml |
| 10 mM |
0.176 ml |
0.878 ml |
1.755 ml |
| 50 mM |
0.035 ml |
0.176 ml |
0.351 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京