UM-164

Catalog No.S8706 Batch:S870601

Technical Data

Formula

C₃₀H₃₁F₃N₈O₃S

Molecular Weight

640.68

CAS No.

903564-48-7

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (156.08 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 Corn oil	0.7mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 14 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMS0 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models NCr/nude mice, 6 weeks of age Dosages 10 mg/kg, 15 mg/kg, or 20 mg/kg Administration i.p.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

Animal Models
NCr/nude mice, 6 weeks of age
Dosages
10 mg/kg, 15 mg/kg, or 20 mg/kg
Administration
i.p.

References

[1] Gilani RA, et al. Clin Cancer Res. 2016, 22(20):5087-5096.

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

UM-164, a Dual Inhibitor of c-Src and p38 MAPK, Suppresses Proliferation of Glioma by Reducing YAP Activity [ Cancers (Basel, 2022, 14(215343)]	PubMed: 36358761

UM-164, a Dual Inhibitor of c-Src and p38 MAPK, Suppresses Proliferation of Glioma by Reducing YAP Activity [ Cancers (Basel, 2022, 14(215343)]

PubMed: 36358761

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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