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

5.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 100 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.

* <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
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