E260

SKU: orb1302693

Description

E260 is a selective small molecule inhibitor targeting the Fer and FerT tyrosine kinases. It is a valuable research tool for studying oncogenic signaling in vitro and has shown potential for investigating therapeutic strategies in cancer models.

Key Properties

• CAS Number: 1241537-79-0
• MW: 438.63
• Purity: 98.52%
• Formula: C₂₄H₃₄N₆S
• SMILES: CC(C)c1ccc(cc1)-c1cn2nc(sc2n1)N1CCC(CN2CCN(C)CC2)CC1
• Target: Fer/FerT kinase,Others
• Solubility: DMSO:Slightly soluble

Bioactivity

• 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 T1/2of 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
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E260, E-260, E 260, Inhibitor, FerT kinase, FerTkinase, Fer and FerT inhibitor, Fer kinase, Fer/FerT kinase, Ferkinase, inhibit

Compound Identifiers

PubChem CID

46898309