product name NVP-BHG712
Description: NVP-BHG712, also known as BHG-712, is an EphB4 inhibitor with IC50 of 25 nM; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.40 μM, 1.27 μM and 1.67 μM, respectively. NVP-BHG712 inhibits EphB4 kinase activity in the low nanomolar range in cellular assays showed high selectivity for targeting the EphB4 kinase when profiled against other kinases in biochemical as well as in cell based assays. BHG-712 shows excellent pharmacokinetic properties and potently inhibits EphB4 autophosphorylation in tissues after oral administration.
References: Angiogenesis. 2010 Sep;13(3):259-67.
503.48
Formula
C26H20F3N7O
CAS No.
940310-85-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 101 mg/mL (200.6 mM)
Water: <1 mg/mL
Ethanol: 3 mg/mL (5.95 mM)
Solubility (In vivo)
NMP+polyethylene glycol 300 (10/90, v/v): 30mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19400863
| In Vitro |
In vitro activity: 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. Kinase Assay: 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. Cell Assay: In Hek293 cells transfected different EphRs, NVP-BHG712 dose-dependently inhibited EphRs autophosphorylation. NVP-BHG712 showed inhibitory preference for EphB4 over EphB2, EphA2, EphB3 and EphA3. |
|---|---|
| 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. |
| Animal model | VEGF-mediated angiogenesis in vivo is induced in a growth factor implant model in mice |
| Formulation & Dosage | Dissolved in 1-Methyl-2-pyrrolidone (NMP) and then diluted with polyethylene glycol 300 (PEG300) to a final concentration of 10% v/v NMP and 90% v/v PEG300.; 30mg/kg; Oral gavage |
| References | Angiogenesis. 2010 Sep;13(3):259-67 |
Related Posts
product name NVP-BHG712
Description: NVP-BHG712, also known as BHG-712, is an EphB4 inhibitor with IC50 of 25 nM; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.40 μM, 1.27 μM and 1.67 μM, respectively. NVP-BHG712 inhibits EphB4 kinase activity in the low nanomolar range in cellular assays showed high selectivity for targeting the EphB4 kinase when profiled against other kinases in biochemical as well as in cell based assays. BHG-712 shows excellent pharmacokinetic properties and potently inhibits EphB4 autophosphorylation in tissues after oral administration.
References: Angiogenesis. 2010 Sep;13(3):259-67.
503.48
Formula
C26H20F3N7O
CAS No.
940310-85-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 101 mg/mL (200.6 mM)
Water: <1 mg/mL
Ethanol: 3 mg/mL (5.95 mM)
Solubility (In vivo)
NMP+polyethylene glycol 300 (10/90, v/v): 30mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19400863
| In Vitro |
In vitro activity: 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. Kinase Assay: 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. Cell Assay: In Hek293 cells transfected different EphRs, NVP-BHG712 dose-dependently inhibited EphRs autophosphorylation. NVP-BHG712 showed inhibitory preference for EphB4 over EphB2, EphA2, EphB3 and EphA3. |
|---|---|
| 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. |
| Animal model | VEGF-mediated angiogenesis in vivo is induced in a growth factor implant model in mice |
| Formulation & Dosage | Dissolved in 1-Methyl-2-pyrrolidone (NMP) and then diluted with polyethylene glycol 300 (PEG300) to a final concentration of 10% v/v NMP and 90% v/v PEG300.; 30mg/kg; Oral gavage |
| References | Angiogenesis. 2010 Sep;13(3):259-67 |