For research use only. Not for therapeutic Use.
UM-164（Cat No.:I014750）is a dual inhibitor that selectively targets p38α MAPK and Src family kinases, which are involved in cell proliferation, differentiation, and survival. By blocking both p38α and Src signaling pathways, UM-164 shows promise in cancer research, particularly in treating aggressive breast cancers like triple-negative breast cancer (TNBC), where these pathways are often dysregulated. Its dual mechanism of action makes it a potent candidate for overcoming resistance to conventional therapies and enhancing the effectiveness of targeted treatments. UM-164 is a valuable tool for studying cancer progression and therapeutic strategies.
| Catalog Number | I014750 |
| CAS Number | 903564-48-7 |
| Synonyms | UM-164; UM 164; UM164.;2-[[6-[4-(2-Hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-5-thiazolecarboxamide |
| Molecular Formula | C30H31F3N8O3S |
| Purity | ≥95% |
| Target | MAPK/ERK Pathway |
| Solubility | Soluble in DMSO |
| IUPAC Name | 2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-1,3-thiazole-5-carboxamide |
| InChI | InChI=1S/C30H31F3N8O3S/c1-18-6-7-22(37-27(43)20-4-3-5-21(14-20)30(31,32)33)15-23(18)38-28(44)24-17-34-29(45-24)39-25-16-26(36-19(2)35-25)41-10-8-40(9-11-41)12-13-42/h3-7,14-17,42H,8-13H2,1-2H3,(H,37,43)(H,38,44)(H,34,35,36,39) |
| InChIKey | ANEBQUSWQAQFQB-UHFFFAOYSA-N |
| 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 |
| Reference | </br>1: Ndagi U, Mhlongo NN, Soliman ME. Emergence of a Promising Lead Compound in the</br> Treatment of Triple Negative Breast Cancer: An Insight into Conformational</br> Features and Ligand Binding Landscape of c-Src Protein with UM-164. Appl Biochem </br> Biotechnol. 2017 Dec 27. doi: 10.1007/s12010-017-2677-z. [Epub ahead of print]</br> PubMed PMID: 29282631.</br>2: Ndagi U, Mhlongo NN, Soliman ME. The impact of Thr91 mutation on c-Src</br> resistance to UM-164: molecular dynamics study revealed a new opportunity for</br> drug design. Mol Biosyst. 2017 May 30;13(6):1157-1171. doi: 10.1039/c6mb00848h.</br> PubMed PMID: 28463369.</br>3: Gilani RA, Phadke S, Bao LW, Lachacz EJ, Dziubinski ML, Brandvold KR, Steffey </br> ME, Kwarcinski FE, Graveel CR, Kidwell KM, Merajver SD, Soellner MB. UM-164: A</br> Potent c-Src/p38 Kinase Inhibitor with In Vivo Activity against Triple-Negative</br> Breast Cancer. Clin Cancer Res. 2016 Oct 15;22(20):5087-5096. Epub 2016 May 6.</br> PubMed PMID: 27154914.</br> </br> |
