Fer and FerT inhibitor
Fer and FerT inhibitor Basic information
- Product Name:
- Fer and FerT inhibitor
- Synonyms:
-
- Fer and FerT inhibitor
- E260
- E260 ;E-260 ;E 260
- 6-(4-Isopropylphenyl)-2-(4-((4-methylpiperazin-1-yl)methyl)piperidin-1-yl)imidazo[2,1-b][1,3,4]thiadiazole
- Imidazo[2,1-b]-1,3,4-thiadiazole, 6-[4-(1-methylethyl)phenyl]-2-[4-[(4-methyl-1-piperazinyl)methyl]-1-piperidinyl]-
- E-260,Inhibitor,E 260,E260,inhibit
- 6-(4-isopropylphenyl)-2-[4-[(4-methylpiperazin-1-yl)methyl]-1-piperidyl]imidazo[2,1-b][1,3,4]thiadiazole
- 1-methyl-4-[(1-{6-[4-(propan-2-yl)phenyl]imidazo[2,1-b][1,3,4]thiadiazol-2-yl}piperidin-4-yl)methyl]piperazine
- CAS:
- 1241537-79-0
- MF:
- C24H34N6S
- MW:
- 438.63
- Mol File:
- 1241537-79-0.mol
Fer and FerT inhibitor Chemical Properties
- Density
- 1.28±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 1 mg/mL (2.28 mM)
- form
- Solid
- pka
- 7.66±0.10(Predicted)
- color
- White to off-white
Fer and FerT inhibitor Usage And Synthesis
Uses
E260 is a Fer/FerT kinase inhibitor.
Biological Activity
E260 (Fer and FerT inhibitor E260), an inhibitor of Fer kinase and FerT, selectively induces metabolic stress in cancer cells by reducing cellular ATP levels by imposing mitochondrial dysfunction and deformation and energy-consuming autophagy.
in vivo
E260 suppresses xenografts progression in vivo. The pharmacokinetic (PK) profile of E260 is determined in mice. E260 exhibits a T 1/2 of 175 min in the blood, and a volume of distribution of 4244 mL/kg suggesting an efficient distribution of the compound in the animal tissues. To evaluate the efficacy of E260 on tumor growth, SW620 cells are subcutaneously introduced into immuno-compromised “Nude” mice. Administration of E260 leads to a significant attenuation of tumor progression throughout the experiment, and to a 10-fold decrease in average tumor volume after 22 days of treatment. To further demonstrate the anti-cancer activity of E260 in vivo, mice bearing SW48 cells derived xenografts are treated with E260 and the tumor progression profiles are determined. Mice treated with E260 demonstrate a 5-6-fold attenuation in tumor progression when compared to the control treated group.
target
| Target | Value |
| Fer kinase () | FerT () |
References
[1] Elkis Y, et al. A novel Fer/FerT targeting compound selectively evokes metabolic stress and necrotic death in malignant cells. Nat Commun. 2017 Oct 16;8(1):940. DOI:10.1038/s41467-017-00832-w
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