JTE-013

SKU: orb1219289

Description

JTE-013 is an effective and specific antagonist of S1P2. JTE-013 suppresses the specific binding of radiolabeled S1P to human and rat S1P2 (IC50s: 17 nM and 22 nM, respectively).JTE-013 is a S1P2 antagonist. JTE-013 (50-200 μM; 1-3 days) decreased cell viability. JTE-013 shows 4.2% inhibition of S1P3 and does not antagonize S1P1 at concentrations up to 10 μM. JTE-013 (10-1000 nM; 30 mins) reverses S1P-induced Akt inhibition and inhibits S1P-induced ERK activation.JTE-013 (gavage; 30 mg/kg daily for 14 consecutive days) decreases tumor size and tumor weight. the modification of JTE-013 to produce the AB1 compound improved potency, intravenous pharmacokinetics, cellular activity, and antitumor activity in NB and may have enhanced clinical and experimental applicability.

Key Properties

• CAS Number: 383150-41-2
• MW: 408.29
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₉Cl₂N₇O
• SMILES: CC(C1=C2C(N(C)N=C2C)=NC(NNC(NC3=CC(Cl)=NC(Cl)=C3)=O)=C1)C
• Target: S1P Receptor
• Solubility: DMSO:100 mg/mL (244.92 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  JTE-013 (gavage; 30 mg/kg daily for 14 consecutive days) reduces tumor size and tumor weight. Animal model: Six-week-old female athymic NCr-nu/nu nude mice. Dosage: 30 mg/kg. Administration: Gavage; daily for 14 consecutive days. Result: Reduced tumor size and tumor weight.
• In Vitro:
  JTE-013 (50-200 μM; 1-3 days) reduces cell viability. JTE-013 (10-1000 nM; 30 mins) reverses S1P-induced Akt inhibition and inhibits S1P-induced ERK activation. JTE-013 displays 4.2% inhibition of S1P3 and does not antagonize S1P1 at concentrations up to 10 μM. Cell Viability Assay Cell line: SK-N-AS cells. Concentration: 50, 100, 150, 200 μ. Incubation time: 1-3 days. Result: Reduced cell viability. Western blot analysis. Cell line: SK-N-AS cells. Concentration: 10, 100, 1000 nM. Incubation time: 30 mins. Result: Reversed S1P-induced Akt inhibition and inhibited S1P-induced ERK activation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

S1P Receptor