(Z)-Semaxinib

SKU: orb1305395

Description

(Z)-Semaxinib (SU5416) is a selective quinolone-based inhibitor of VEGFR2 (Flk-1/KDR) with an IC50 of 1.23 μM, exhibiting over 20-fold selectivity against PDGFRβ and no activity on FGFR, InsR, or EGFR. This antineoplastic agent has been utilized in research to study angiogenesis and tumor growth in both cellular assays and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 194413-58-6
• MW: 238.28
• Purity: 99.99%
• Formula: C₁₅H₁₄N₂O
• SMILES: C(=C\1/C=2C(NC1=O)=CC=CC2)\C=3NC(C)=CC3C
• Target: c-Met/HGFR,VEGFR
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:7.14 mg/mL (29.96 mM);Ethanol:2 mg/mL (8.39 mM)

Bioactivity

• Target IC50:
  VEGFR2/Flk1:1.23 μM
• In Vivo:
  Semaxanib demonstrates dose-dependent inhibition of VEGF (IC50: 0.04 μM) and FGF (IC50: 50 μM) induced mitosis. It does not affect the growth of C6 glioma, Calu 6 lung cancer, A375 melanoma, A431 squamous cell carcinoma, and SF767T glioblastoma cells in vitro (IC50s > 20 μM). Additionally, Semaxanib inhibits VEGF-dependent phosphorylation of the Flk-1 receptor in NIH 3T3 cells overexpressing Flk-1 (IC50: 1.04 μM) and inhibits PDGF-dependent autophosphorylation in NIH 3T3 cells (IC50: 20.3 μM).
• In Vitro:
  In tests conducted on ten tumor cell lines, Semaxanib significantly inhibited subcutaneous growth in eight of them (A431, Calu-6, C6, LNCAP, EPH4-VEGF, 3T3HER2, 488 g2M2, and SF763T cells) with an average mortality rate of 2.5%. The compound demonstrated a dose-dependent suppression of in vivo A375 tumor growth. Administered at 25 mg/kg/day, Semaxanib exhibited potent anti-angiogenic activity, significantly reducing the overall functional vascular density of the tumor microvasculature. Furthermore, Semaxanib (i.p.) inhibited more than 85% of subcutaneous tumor growth without any detectable toxicity.
• Cell Research:
  HUVECs are plated in 96-well, flat-bottomed plates (1×104 cells/100 μL/well) in F-12K media containing 0.5% heat-inactivated FBS and cultured at 37 ℃ for 24 h to quiesce the cells. Serial dilutions of compounds prepared in medium containing 1% DMSO are then added for 2 h, followed by the addition of mitogenic concentrations of either VEGF at 5 ng/mL or 20 ng/mL or acidic fibroblast growth factor at 0.25–5 ng/mL in media. The final concentration of DMSO in the assay is 0.25%. After 24 h, either [3H]thymidine (1 μCi/well) or BrdUrd is added, and the cell monolayers are incubated for another 24 h. The uptake of either [3H]thymidine or BrdUrd into cells is quantitated using a liquid scintillation counter or a BrdUrd ELISA, respectively.(Only for Reference)

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

cytotoxicity, c-Met/HGFR, (Z) Semaxinib, (Z)-Semaxanib, (Z)Semaxinib, (Z)-SU5416, HepG2 cells, Inhibitor, inhibit, Semaxinib, TAMH cells, SU5416, SU-5416, SU 5416, VEGFR2/Flk1

Compound Identifiers

PubChem CID

5329098