Ningetinib Tosylate

SKU: orb1218860

Description

Ningetinib Tosylate is an orally bioavailable tyrosine kinase inhibitor with IC50s of <1.0, 1.9 and 6.7 nM for Axl, VEGFR2, and c-Met, respectively.

Key Properties

• CAS Number: 1394820-77-9
• MW: 728.79
• Purity: >98% (HPLC)
• Formula: C₃₈H₃₇FN₄O₈S
• SMILES: O=C(C1=C(C)N(C)N(C2=CC=CC=C2)C1=O)NC3=CC=C(OC4=CC=NC5=CC(OCC(C)(O)C)=CC=C45)C(F)=C3.CC6=CC=C(S(=O)(O)=O)C=C6
• Target: TAM Receptor
• Solubility: DMSO:8 mg/mL (10.98 mM; Need ultrasonic and warming)

Bioactivity

• In Vivo:
  When single dosed orally (3 mg/kg) to U87MG tumor-bearing nude mice, Ningetinib Tosylate (CT053PTSA) 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 orthotopic U87MG human glioblastoma xenograft model, Ningetinib Tosylate prolongs the median survival time (MST) and yields significant increase in life-span value (ILS = 32%, p = 0.003) at an oral dose of 20 mg/kg/day (dosed 21 days) versus the vehicle-treated group.
• In Vitro:
  Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. In cell-based functional assays, Ningetinib Tosylate (CT053PTSA) inhibits HGF and VEGF-stimulated HUVEC proliferation and microvascular angiogenesis in rat aortic rings with IC50 values of 8.6 and 6.3 nM, respectively.

Storage & Handling

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

Quick Database Links

Gene Symbol

TAM Receptor