Ningetinib

SKU: orb1296265

Description

Ningetinib (CT-053) is a potent, orally active small molecule inhibitor targeting Axl, VEGFR2, and c-Met kinases with low nanomolar IC50 values. It is utilized in preclinical cancer research, particularly in studies investigating tumor angiogenesis, metastasis, and resistance mechanisms in both cellular and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1394820-69-9
• MW: 556.58
• Purity: 99.98% (May vary between batches)
• Formula: C₃₁H₂₉FN₄O₅
• SMILES: Cc1c(C(=O)Nc2ccc(Oc3ccnc4cc(OCC(C)(C)O)ccc34)c(F)c2)c(=O)n(-c2ccccc2)n1C
• Target: VEGFR,TAM Receptor,c-Met/HGFR
• Solubility: DMSO:15 mg/mL (26.95 mM)

Bioactivity

• Target IC50:
  VEGFR2:1.9 nM (cell free)|Axl:<1 nM (cell free)|c-Met:6.7 nM (cell free)
• In Vivo:
  In the orthotopic U87MG human glioblastoma xenograft model, Ningetinib prolongs the median survival time and yields a significant increase in life-span value (ILS=32%) at an oral dose of 20 mg/kg/day (dosed 21 days) versus the vehicle-treated group. When single dosed orally (3 mg/kg) to U87MG tumor-bearing nude mice, Ningetinib potently inhibits the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 for up to 6 hours in tumor tissues.
• In Vitro:
  In cell-based functional assays, Ningetinib inhibits VEGF and HGF-stimulated HUVEC proliferation and microvascular angiogenesis in rat aortic rings with IC50 values of 6.3 and 8.6 nM, respectively.

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, Ningetinib, HGFR, Inhibitor, Mer, AXL, Axl, cMet, cMet/HGFR, c-Met, c-Met/HGFR, CT053, CT-053, CT053PTSA, CT 053, TAM Receptor, TAMReceptor, Tyro3, VEGFR2, VEGFR, Vascular endothelial growth factor receptor

Compound Identifiers

PubChem CID

60165029