Ningetinib Tosylate

SKU: orb1296250

Description

Ningetinib Tosylate is a potent, orally active small molecule inhibitor targeting Axl, VEGFR2, and c-Met kinases with IC50 values below 10 nM. It is utilized in preclinical cancer research, particularly in studies involving tumor angiogenesis, metastasis, and resistance mechanisms in both cellular and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1394820-77-9
• MW: 728.79
• Purity: 99.77% (May vary between batches)
• Formula: C₃₈H₃₇FN₄O₈S
• SMILES: Cc1ccc(cc1)S(O)(=O)=O.Cc1c(C(=O)Nc2ccc(Oc3ccnc4cc(OCC(C)(C)O)ccc34)c(F)c2)c(=O)n(-c2ccccc2)n1C
• Target: TAM Receptor|||c-Met/HGFR|||VEGFR
• Solubility: DMSO:8 mg/mL (10.98 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.37 mM)

Bioactivity

• Target IC50:
  c-Met:6.7 nM (cell free)|Axl:<1 nM (cell free)|VEGFR2:1.9 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.
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• 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.
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Storage & Handling

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

Alternative Names

cMet, c-Met, cMet/HGFR, c-Met/HGFR, AXL, Axl, HGFR, Mer, inhibit, Inhibitor, Ningetinib, Ningetinib Tosylate, TAM Receptor, TAMReceptor, Vascular endothelial growth factor receptor, VEGFR, VEGFR2, Tyro3

Compound Identifiers

PubChem CID

73442844