Home Protein Tyrosine Kinase Src inhibitor - p38 MAPK inhibitor UM-164 For research use only.

UM-164

UM-164 is a highly potent, dual c-Src/p38inhibitor of c-Src with a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β.

UM-164 Chemical Structure

UM-164 Chemical Structure

CAS: 903564-48-7

Selleck's UM-164 has been cited by 1 publication

Purity & Quality Control

Batch: S870601 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.12%
99.12

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Biological Activity

Description UM-164 is a highly potent, dual c-Src/p38inhibitor of c-Src with a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β.
Targets
p38α [1] p38β [1] c-Src [1]
(Cell-free assay)
2.7 nM(Kd)
In vitro
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.[1].
Cell Research Cell lines MDA-MB 468 cells
Concentrations 5 μM
Incubation Time 4 h
Method

MDA-MB 468 cells were trypsinized and allowed to adhere overnight in a 6-well plate. Cells were then treated with 5 μmol/L dasatinib, 5 μmol/L UM-164, or vehicle (DMSO) for 4 hours. Cells were then fixed with 4% paraformaldehyde for 15 minutes at room temperature followed by three washes with PBS. The fixed cells were treated with 1 μmol/L of an irreversible turn-on Src fluorophore for 1 hour followed by three washes with PBS. Cells were then mounted on slides and stored for 30 minutes at 4°C in the dark. Imaging was performed.
In Vivo
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[1].
Animal Research Animal Models NCr/nude mice, 6 weeks of age
Dosages 10 mg/kg, 15 mg/kg, or 20 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 640.68 Formula

C30H31F3N8O3S
CAS No. 903564-48-7 SDF --
Smiles CC1=C(C=C(C=C1)NC(=O)C2=CC(=CC=C2)C(F)(F)F)NC(=O)C3=CN=C(S3)NC4=CC(=NC(=N4)C)N5CCN(CC5)CCO
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (156.08 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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