MGCD-265 analog


CAS No. : 875337-44-3

875337-44-3
Price and Availability of CAS No. : 875337-44-3
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5mg $100 In-stock
10mg $160 In-stock
25mg $340 In-stock
50mg $540 In-stock
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Cat. No. : HY-10991
M.Wt: 517.60
Formula: C26H20FN5O2S2
Purity: >98 %
Solubility: DMSO : ≥ 100 mg/mL
Introduction of 875337-44-3 :

MGCD-265 analog is a potent and oral active inhibitor of c-Met and VEGFR2 tyrosine kinases, with IC50s of 29 nM and 10 nM, respectively. MGCD-265 analog has significant antitumor activity[1]. IC50 & Target: IC50: 29 nM (c-Met), 10 nM (VEGFR2)[1] In Vitro: MGCD-265 analog inhibits A549 cells migration and DU145 cells scattering, with IC50s of 0.4 μM and 0.08 μM, respectively, in HGF-driven cell migration and scattering assays[1].
MGCD-265 analog inhibits HUVEC ERK phosphorylation (IC50=0.03 μM) and HUVEC proliferation (IC50=0.006 μM) in VEGF-dependent cell-based assays[1].
In Vivo: MGCD-265 analog (20 mg/kg; p.o.) inhibits tumor growth inhibition on various human tumor models in mice[1].
MGCD-265 analog exhibits moderate oral bioavailability (rat 12%, dog 42%) and Cmax (rat 0.14, dog 0.21 uM/(mg/kg)) following oral administration (rat 5-25, dog 5 mg/kg)[1].
MGCD-265 analog exhibits reasonable terminal elimination half-lives (rat 1.2, dog 5.8 h) due to plasma clearance (rat 0.33, dog 1.1 L/(kg h)) following intravenous administration (rat 2.5, dog 0.8 mg/kg) [1].

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