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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
中文名称
UM-164
英文名称
UM-164
中文别名
-
英文别名
5-​Thiazolecarboxamide,2-​[[6-​[4-​(2-​hydroxyethyl)​-​1-​piperazinyl]​-​2-​methyl-​4-​pyrimidinyl]​amino]​-​N-​[2-​methyl-​5-​[[3-​(trifluoromethyl)​benzoyl]​amino]​phenyl]​-
CAS号
903564-48-7
分子式
C30H31F3N8O3S
分子量
640.68 g/mol
精确质量
10mM in DMSO
PSA
164.000 Ų
Logp
4.501
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MedMol UM-164 99% 50mg

品牌:MedMol
货号:S88743-50mg
级别: -
货期:30天
已售 77 件
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