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Glesatinib MGCD-265 analog

Glesatinib MGCD-265 analog 875337-44-3
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Chemical Information
Product name:Glesatinib MGCD-265 analog Purity:98% min
CAS NO:875337-44-3 Solubility:10 mM in DMSO
Molecular Formula:C26H20FN5O2S2 Package:Package according to customer requirements
Molecular Weight:517.598 Storage:Store at -20℃
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Remarks
MGCD-265-analog (structurally related to MGCD-265) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively. IC50 value:10 nM (VEGFR2), 29 nM(c-Met) [1] Target:VEGFR, c-Met in vivo: MGCD-265-analog has a reasonable half-life, 1.2 h in rats and 5.8 h in dogs, and has an acceptable clearance, 0.33 L/(kg h) in rats and 1.1 L/(kg h) in dogs. The steady state volume of distribution was low in rats (0.25 L/kg) and reasonable in dogs (1.5 L/kg), while the oral bio-availability was determined to be 12% and 42% in rats and dogs, respectively. GCD-265-analog performed well in vivo against a panel of different human tumor types, particularly those that are driven by or overexpress c-Met (MNNGHOS and MKN45). Tumor growth inhibition at a dose of 20 mg/kg po once daily ranged from 41% to 94%. MGCD-265-analog was found to show spill-over inhibition of a number of kinases in addition to the intended c-Met/VEGFR2 activity. MGCD-265-analog has significant antitumor activity in vivo.
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