Tie2 kinase inhibitor

SKU: orb1223545

Description

Tie2 kinase inhibitor is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 948557-43-5
• MW: 439.53
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₁N₃O₂S
• SMILES: O=S(C1=CC=C(C2=NC(C3=CC=C4C=C(OC)C=CC4=C3)=C(C5=CC=NC=C5)N2)C=C1)C
• Target: Tie-2
• Solubility: DMSO:35 mg/mL (79.63 mM); Ethanol:<1 mg/mL (<1 mM); Water:<1 mg/mL (<1 mM)

Bioactivity

• In Vivo:
  Tie2 kinase inhibitor 1 (intraperitoneally; 50 mg/kg; twice a week for 6 weeks) results in statistically significant reductions in tumor volume by day 15. Tie2 kinase inhibitor 1 results in a 61% reduction in tumor volume by day 20, and reduces tumor volume by 45% by 6 weeks. Animal model: Athymic nude mice (6-to 8-week-old females). Dosage: 50 mg/kg. Administration: Intraperitoneally; twice a week for 6 weeks. Result: Resulted in statistically significant reductions in tumor volume.
• In Vitro:
  Tie2 kinase inhibitor 1 (compound 5) has an IC50 of 50 μM for p38 and has moderate to excellent cellular activities (cell IC50 = 232 nM). Tie2 kinase inhibitor 1 inhibits tunica internal endothelial cell kinase 2 (Tie2).

Storage & Handling

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

Alternative Names

Tunica Interna Endothelial Cell Kinase 2 Inhibitor

Quick Database Links

Gene Symbol

Tie-2