Lenvatinib (E7080) 417716-92-8
Product Description
Molecular Weight: 426.85 Lenvatinib (E7080) is a Multi-Target Inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β. Phase 3.
Biological Activity
E7080, as a Potent Inhibitor of in vitro Angiogenesis, shows a
significantly inhibitory effect on VEGF/KDR and SCF/Kit signaling.
According to the in vitro receptor tyrosine and serine/threonine kinase
assays, E7080 inhibits Flt-1, KDR, Flt-4 with IC50 of 22, 4.0 and 5.2
nM,respectively.
In addition to these kinases, E7080 also inhibits
FGFR1 and PDGFR tyrosine kinases with IC50 value of 46, 51 and 100 nM
for FGFR1, PDGFRα and PDGFRβ, respectively. E7080
potently inhibits phosphorylation of VEGFR2 (IC50, 0.83 nM) and VEGFR3
(IC50, 0.36 nM) in HUVECs which is stimulated by VEGF and VEGF-C,
respectively.
A recent study shows that E7080 treatment
(both at 1 μM and 10 μM) results in a significant inhibition of cell
migration and invasion by inhibiting FGFR and PDGFR signaling.
When orally administrated in a H146 xenograft model, E7080 inhibits the
growth of H146 tumor at 30 and 100 mg/kg in a dose-dependent manner and
leads to tumor regression at 100 mg/kg. Furthermore, E7080 at 100 mg/kg
decreases microvessel density more than anti-VEGF antibody and imatinib
treatment.
[E7080 significantly inhibits local tumor
growth in a MDA-MB-231 mammary fat pad (m.f.p.) model with RTVs
(calculated tumor volume on day 8/tumor volume on day 1) of 0.81, and
reduces both angiogenesis and lymphangiogenesis of established
metastatic nodules of MDA-MB-231 tumor in the lymph nodes.
Contact us if you need more details on 417716-92-8. We are ready to answer your questions on packaging, logistics, certification or any other aspects about Lenvatinib 417716-92-8、E7080 417716-92-8. If these products fail to match your need, please contact us and we would like to provide relevant information.
Biological Activity
E7080, as a Potent Inhibitor of in vitro Angiogenesis, shows a
significantly inhibitory effect on VEGF/KDR and SCF/Kit signaling.
According to the in vitro receptor tyrosine and serine/threonine kinase
assays, E7080 inhibits Flt-1, KDR, Flt-4 with IC50 of 22, 4.0 and 5.2
nM,respectively.
In addition to these kinases, E7080 also inhibits
FGFR1 and PDGFR tyrosine kinases with IC50 value of 46, 51 and 100 nM
for FGFR1, PDGFRα and PDGFRβ, respectively. E7080
potently inhibits phosphorylation of VEGFR2 (IC50, 0.83 nM) and VEGFR3
(IC50, 0.36 nM) in HUVECs which is stimulated by VEGF and VEGF-C,
respectively.
A recent study shows that E7080 treatment
(both at 1 μM and 10 μM) results in a significant inhibition of cell
migration and invasion by inhibiting FGFR and PDGFR signaling.
When orally administrated in a H146 xenograft model, E7080 inhibits the
growth of H146 tumor at 30 and 100 mg/kg in a dose-dependent manner and
leads to tumor regression at 100 mg/kg. Furthermore, E7080 at 100 mg/kg
decreases microvessel density more than anti-VEGF antibody and imatinib
treatment.
[E7080 significantly inhibits local tumor
growth in a MDA-MB-231 mammary fat pad (m.f.p.) model with RTVs
(calculated tumor volume on day 8/tumor volume on day 1) of 0.81, and
reduces both angiogenesis and lymphangiogenesis of established
metastatic nodules of MDA-MB-231 tumor in the lymph nodes.
Contact us if you need more details on 417716-92-8. We are ready to answer your questions on packaging, logistics, certification or any other aspects about Lenvatinib 417716-92-8、E7080 417716-92-8. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : Protein Tyrosine Kinase > VEGFR Inhibitor
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