Semaxinib

SKU: orb1306586

Description

Semaxinib

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 204005-46-9
• MW: 238.28
• Purity: 99.84%
• Formula: C₁₅H₁₄N₂O
• SMILES: C(=C1C=2C(NC1=O)=CC=CC2)C=3NC(C)=CC3C
• Target: VEGFR
• Solubility: DMSO:2.39 mg/mL (10.03 mM)

Bioactivity

• Target IC50:
  VEGFR2:1.23 μM
• In Vivo:
  Administering SU5416 daily (i.p., 3 mg/kg/day) effectively inhibits C6 tumor growth in the colon, achieving a growth inhibition of 62% by day 16 (P=0.001), comparable to the 54% inhibition in the hindflank by day 18 (P=0.001). This demonstrates SU5416's potential to suppress tumor development in various locations, possibly due to differences in preexisting vasculature. Further, a higher dose of SU5416 (25 mg/kg) significantly reduces tumor growth rates, with tumors being only 8% the size of those in control animals by day 22, primarily through a substantial decrease in the area covered by newly formed glioma microvasculature in treated animals, suggesting a minimized initial tumor vascularization.
• In Vitro:
  SU5416 inhibits VEGF-driven mitogenesis in a dose-dependent manner with an IC50 of 0.04±0.02 μM (n=3). In contrast, SU5416 blocked FGF-dependent mitogenesis of HUVECs with an IC50 of 50 μM (n=10). The selective activity of SU5416 on Flk-1 is supported by the fact that testing of SU5416 using NIH 3T3 cells overexpressing either the EGF or insulin receptors indicated a complete lack of activity (IC50>100 μM). This observation is confirmed by immunoblotting after ligand stimulation. An IC50 of 20.26±5.2 μM (n=7), which is about 20-fold less in potency on PDGF-dependent autophosphorylation, is observed when SU5416 is tested in NIH 3T3 cells overexpressing the human PDGF receptor β.
• Cell Research:
  SU5416 is dissolved in DMSO and stored,and then diluted with appropriate media (DMSO<0.5%) before use 3T3Her2 and 488 g2M2 are NIH3T3 fibroblast cell lines engineered to overexpress Her2 and to express human PDGF-BB and human PDGF receptor β.Both cell lines are cultured in DMEM supplemented with 2% CS and 2 mM L-glutamine.C6,Calu 6,A375,A431,and SF767T are plated in their respective growth medium at 2×103 cells/100 μL/well in 96-well,flat-bottomed plates.SU5416 is serially diluted in media containing DMSO (<0.5%) and added to cultures of tumor cells 1 day after the initiation of culture.Cell growth is measured after 96 h using the sulforhodamine B method.IC50s are calculated by curve fitting using four-parameter analysis.

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

inhibit, Inhibitor, Flk1, Vascular endothelial growth factor receptor, VEGFR, Semaxinib, SU 5416, SU5416, SU-5416

Compound Identifiers

PubChem CID

123015