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NVP-BHG712

Chemical Structure : NVP-BHG712

CAS No.: 940310-85-0

NVP-BHG712 (NVP-BHG 712;NVP BHG 712)

Catalog No.: PC-43438Not For Human Use, Lab Use Only.

NVP-BHG712 is a potent, specific inhibitor of EphB4 kinase that inhibits EphB4 autophosphorylation with IC50 of 25 nM in cell-bases assays, displays little to no activity against VEGFR2, IGF1R and InsR.

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Biological Activity

NVP-BHG712 is a potent, specific inhibitor of EphB4 kinase that inhibits EphB4 autophosphorylation with IC50 of 25 nM in cell-bases assays, displays little to no activity against VEGFR2, IGF1R and InsR.
NVP-BHG712 dose dependently inhibits autophosphorylation of the EphRs, showing some preference for EphB4 followed by inhibition of EphB2, EphA2, EphB3 and EphA3.
NVP-BHG712 shows excellent pharmacokinetic properties and potently inhibits EphB4 autophosphorylation in tissues after oral administration, inhibits VEGF driven tissue growth and angiogenesis in vivo.

Physicochemical Properties

M.Wt 503.48
Formula C26H20F3N7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzamide, 4-methyl-3-[[1-methyl-6-(3-pyridinyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]amino]-N-[3-(trifluoromethyl)phenyl]-

References

1. Martiny-Baron G, et al. Angiogenesis. 2010 Sep;13(3):259-67.

2. Kathawala RJ, et al. Oncotarget. 2015 Jan 1;6(1):510-21.

3. Wnuk M, et al. Kidney Int. 2012 Jun;81(12):1212-25.

4. Becerikli M, et al. Int J Cancer. 2015 Apr 15;136(8):1781-91.

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