Description
As a multi-target inhibitor, MGCD-265 can inhibit Met, VEGFR1, VEGFR2, VEGFR3, Ron, and Tie2 with IC50 of 1 nM, 3 nM, 3 nM, 4 nM, 2 nM, and 7 nM.
Storage
2 years at -20 centigrade
Targets
VEGFR1/VEGFR2/VEGFR3, Ron, Tie2, c-Met,
Molecular Formula
C26H20FN5O2S2
Solubility
DSMO 104 mg/mL Water
In vitro
As a multi-target inhibitor, MGCD-265 can inhibit Met, VEGFR1, VEGFR2, VEGFR3, Ron, and Tie2 with IC50 of 1 nM, 3 nM, 3 nM, 4 nM, 2 nM, and 7 nM. MGCD-265 can inhibit Met phosphorylation in Met amplified cell and VEGFR2 phosphorylation with IC50 of 20 nM and 30 nM. MGCD-265 shows inhibition to cell lines including MKN45, MNNG-HOS, SNU-5, HCT116 and MDA-MB-231. By inhibiting c-Met phosphorylation, MGCD-265 can block the downstream signaling pathways of c-MET.
In vivo
In vivo, the combination of MGCD265 (10 mg/kg) and erlotinib (50 mg/kg) can result in tumor regression in a grastic tumor xenograft model. Combinatoin of MGCD265 and erlotinib regulate genes involved in tumor cell proliferation and apoptosis. And the the combination of MGCD265 and erlotinib in the MKN45 deregulate the RNA level of gene involved in glycolysis.
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