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E260

Catalog No. T4638   CAS 1241537-79-0
Synonyms: Fer and FerT inhibitor

E260 (Fer and FerT inhibitor) is a Fer/FerT kinase inhibitor

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E260 Chemical Structure
E260, CAS 1241537-79-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 135.00
5 mg In stock $ 289.00
10 mg In stock $ 455.00
25 mg In stock $ 753.00
50 mg In stock $ 1,060.00
100 mg In stock $ 1,430.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description E260 (Fer and FerT inhibitor) is a Fer/FerT kinase inhibitor
In vitro Fer and FerT inhibitor, which selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level. When applied to metastatic grade IV SW620 CC cells, which are serum starved for 16 h and treated with 3 mM H2O2 to activate Fer,Fer and FerT inhibitor exhibits inhibitory effects on the Fer-kinase activity as is reflected by suppressed auto-phosphorylation activity of the enzyme.
In vivo Fer/FerT kinase inhibitor suppresses xenografts progression in vivo. The pharmacokinetic (PK) profile of Fer/FerT kinase inhibitor is determined in mice. Fer/FerT kinase inhibitor exhibits a T1/2?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 Fer/FerT kinase inhibitor on tumor growth, SW620 cells are subcutaneously introduced into immuno-compromised "Nude" mice. Administration of Fer/FerT kinase inhibitor 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 Fer/FerT kinase inhibitor in vivo, mice bearing SW48 cells derived xenografts are treated with Fer/FerT kinase inhibitor and the tumor progression profiles are determined. Mice treated with Fer/FerT kinase inhibitor demonstrate a 5-6-fold attenuation in tumors progression when compared to the control treated group
Synonyms Fer and FerT inhibitor
Molecular Weight 438.63
Formula C24H34N6S
CAS No. 1241537-79-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Slightly soluble

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library NO PAINS Compound Library Bioactive Compounds Library Max Kinase Inhibitor Library Bioactive Compound Library

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Keywords

E260 1241537-79-0 Others Fer/FerT kinase E 260 Inhibitor Fer and FerT inhibitor inhibit E-260 inhibitor

 

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