aladdin 阿拉丁 U414125 UM-164 903564-48-7 99%

中文名：UM-164

英文名：UM-164

纯度：≥99%

货号：U414125

Cas号：903564-48-7

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

UM-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.

Targets

p38α ; p38β ; c-Src (Cell-free assay) ; 2.7 nM(Kd)

In vitro

UM-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 vivo

In 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 

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