NVP-BHG712 is an oral active EphB4 kinase autophosphorylation inhibitor, with IC50 values of 3.3 nM and 3.0 nM for EphA2 and EphB4, respectively.
体外研究
NVP-BHG712 inhibits VEGF driven vessel formation, while it has only little effects on VEGF receptor (VEGFR) activity. The data suggests a close cross talk between the VEGFR and EphR signaling during vessel formation.
体内研究
NVP-BHG712 (3, 10 and 30 mg/kg, p.o., daily) inhibits VEGF driven tissue growth and angiogenesis.
Animal Model:
Mice arrying chambers.
Dosage:
3, 10 and 30 mg/kg.
Administration:
P.O. daily for 4 days.
Result:
Significantly inhibited VEGF stimulated tissue formation and vascularization at doses of daily 3 mg/kg. Administration of 10 mg/kg/kg p.o. was sufficient to reverse VEGF enhanced tissue formation and vessel growth.
分子式
C26H20F3N7O
分子量
503.48
CAS号
940310-85-0
运输条件
Room temperature in continental US; may vary elsewhere.