| 产品描述： | p38α 选择性抑制剂;p38α Selective Inhibitors;;InformationUM-164 is a highly potent, dualc-Src/p38inhibitor ofc-Srcwith a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β.Targetsp38α ; p38β ; c-Src (Cell-free assay) ; 2.7 nM(Kd)In vitroUM-164 binds the inactive kinase conformation of c-Src. UM-164 alters the cell localization of c-Src in TNBC (anti-triple-negative breast cancer) cells. It has potent antiproliferative activity (average GI50 = 160 nmol/L) in all TNBC cell lines tested. UM-164 is a potent inhibitor of p38α and p38β. p38 MAPK phosphorylation is completely absent in SUM 149 cells treated with 50 nmol/L of UM-164. UM-164 can suppress both cell motility and invasion of MDA-MB 231 and SUM 149 cell lines with an IC50 = 50 nmol/L. FAK phosphorylation is inhibited by UM-164 in SUM 149 cells. UM-164 also efficiently reduces activation of EGFR (at both Tyr-845 and Tyr-1068), AKT, and ERK1/2, all of which are not direct targets of UM-164..In vivoIn xenograft models of TNBC (anti-triple-negative breast cancer), UM-164 results in a significant decrease of tumor growth compared with controls, with limited in vivo toxicity.Cell Research(from reference)Cell lines：MDA-MB 468 cells Concentrations：5 μM Incubation Time：4 h |
| 体内研究： |
A xenograft study is performed using NCr/nude mice implanted with MDA-MB 231 and SUM 149 cell lines. Once the tumors become palpable, the mice are randomized into control and treatment groups. Mice are injected intraperitoneally with either drug (10 and 20 mg/kg in both xenograft studies; a 15 mg/kg dose is added to the SUM 149 xenograft studies) or vehicle every other day (n=5 for each group). At the selected doses of UM-164, there is no significant weight loss or gross abnormalities observed in the treated animals, even after 52 days of treatment. However, tumor growth is significantly inhibited in both the 10 mg/kg and 20 mg/kg dose groups compared with the vehicle-treated group (P<0.026 and P<0.004, respectively). |
| 参考文献： |
1. Gilani RA, et al. UM-164: A Potent c-Src/p38 Kinase Inhibitor with In Vivo Activity against Triple-Negative Breast Cancer. Clin Cancer Res. 2016 Oct 15;22(20):5087-5096. |
| 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 |
1.561 ml |
7.804 ml |
15.608 ml |
| 5 mM |
0.312 ml |
1.561 ml |
3.122 ml |
| 10 mM |
0.156 ml |
0.78 ml |
1.561 ml |
| 50 mM |
0.031 ml |
0.156 ml |
0.312 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。 |
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