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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UM-164
Dangerous GoodsCAS number:903564-48-7 molecular formula:C30H31F3N8O3S
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compound introduction
Specs
| Chinese alias | - | ||
| English alias | 5-Thiazolecarboxamide,2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]- | ||
| CAS number | 903564-48-7 | molecular formula | C30H31F3N8O3S |
| molecular weight | 640.68 g/mol | Exact mass | 10mM in DMSO |
| PSA | 164.000 Ų | logp | 4.501 |
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Safety information
pictogram:
GHS07
Signal word:
Warning
Hazard Statement:
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激
Statement of Preventive Measures:
P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染:用水充分清洗。 P264: 处理后要彻底洗手。 P337+P313: 如仍觉眼刺激:求医/就诊。 P362+P364: 脱掉沾污的衣服,清洗后方可重新使用。 P332+P313: 如发生皮肤刺激:求医/就诊。
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