[CAS NO. 903564-48-7] UM-164
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PRODUCTS SPECIFICATIONS [903564-48-7]
Store
Catalog
SLK-S8706
Brand
Selleck
CAS
903564-48-7
DESCRIPTION [903564-48-7]
Overview
| MDL | MFCD31692378 |
|---|---|
| Molecular Weight | 640.68 |
| Molecular Formula | C30H31F3N8O3S |
| SMILES | O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCO)CC3)=C2)S1)NC4=CC(NC(C5=CC=CC(C(F)(F)F)=C5)=O)=CC=C4C |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5608 mL | 7.8042 mL | 15.6084 mL |
| 5 mM | 0.3122 mL | 1.5608 mL | 3.1217 mL |
| 10 mM | 0.1561 mL | 0.7804 mL | 1.5608 mL |
| 50 mM | 0.0312 mL | 0.1561 mL | 0.3122 mL |
Description
UM-164 is a highly potent, dual inhibitor of with a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β.
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.
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