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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关键字： 5-Thiazolecarboxamide,2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-
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