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Ningetinib

Cat. No. M10329
Ningetinib Structure
Synonym:

CT-053; DE-120; CT053PTSA

Size Price Availability Quantity
10mg USD 160  USD160 In stock
25mg USD 300  USD300 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Ningetinib is a potent, orally bioavailable tyrosine kinase inhibitor for Axl, VEGFR2 and c-Met with IC50 values of <1.0, 1.9 and 6.7 nM, respectively. Ningetinib (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. 

In vivo, Ningetinib (3 mg/kg; orally) treatment on U87MG tumor-bearing nude mice potently inhibits the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 for up to 6 hours in tumor tissues.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 556.58
Formula C31H29FN4O5
CAS Number 1394820-69-9
Purity >99%
Solubility DMSO 18 mg/mL
Storage at -20°C
References

[1] Lu Liu, et al. Br J Clin Pharmacol. Drug interaction of ningetinib and gefitinib involving CYP1A1 and efflux transporters in non-small cell lung cancer

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Ningetinib, CT-053; DE-120; CT053PTSA supplier, VEGFR/PDGFR, inhibitors

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