UM-164

For research use only.

Catalog No.S8706

UM-164 Chemical Structure

Molecular Weight(MW): 640.68

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.

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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

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].

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].

Protocol

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: NCr/nude mice, 6 weeks of age
  • Dosages: 10 mg/kg, 15 mg/kg, or 20 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (156.08 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 640.68
Formula

C30H31F3N8O3S

CAS No. 903564-48-7
Storage powder
in solvent
Synonyms N/A
Smiles CC1=NC(=CC(=N1)NC2=NC=C(S2)C(=O)NC3=CC(=CC=C3C)NC(=O)C4=CC(=CC=C4)C(F)(F)F)N5CCN(CCO)CC5

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID