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Products are for research use only. Not for human use. We do not sell to patients.
(NVP-BHG 712; NVP BHG 712)
NVP-BHG712 Chemical Structure
|Product name: NVP-BHG712|
|Cat. No.: HY-13258|
NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
IC50 value: 25 nM(EC50)
Target: EphB4 receptor;c-Raf; c-Src
in vitro: NVP-BHG712 treatment also dose dependently leads to the inhibition of RTK autophosphorylation in stable transfected A375 melanoma cells with EC50 of 25 nM and 4.2 μM for EphB4 and VEGFR2, respectively .
in vivo: In a growth factor-induced angiogenesis model, NVP-BHG712 (3 mg/kg, p.o) significantly suppresses VEGF stimulated tissue formation and vascularization by inhibiting EphB4 forward signaling. Furthermore, NVP-BHG712 (10 mg/kg/kg, p.o.) potently reverses VEGF enhanced tissue formation and vessel growth. NVP-BHG712 (3 mg/kg, p.o.) shows a long lasting exposure with concentrations around 10 μM in plasma as well as in lung and liver tissue for up to 8 hours, and thus results in a long lasting inhibition of EphB4 kinase activity in mice .
|M.Wt||503.48||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO ≥100mg/mL Water <1.2mg/mL Ethanol ≥35mg/mL
|1 mg||5 mg||10 mg|
|1 mM||1.9862 mL||9.9309 mL||19.8618 mL|
|5 mM||0.3972 mL||1.9862 mL||3.9724 mL|
|10 mM||0.1986 mL||0.9931 mL||1.9862 mL|
ALW-II-41-27 is a novel Eph receptor tyrosine kinase inhibitor.
JI-101 is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor (beta) (PDGFR-(beta)), and ephrin type-B receptor 4 (EphB4). JI-101 inhibits angiogenesis, and subsequently tumor growth.