Uses
NVP-BHG712 is a small molecule specific EphB4, VEGFR2, c-raf, c-src and c-Abl kinase inhibitor with ED50 of 25 nM, 4.2, 0.4, 1.3 and 1.7μM, respectively.
Definition
ChEBI: 4-methyl-3-[[1-methyl-6-(3-pyridinyl)-4-pyrazolo[3,4-d]pyrimidinyl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide is a member of benzamides.
Biochem/physiol Actions
NVP-BHG712 is a very potent, selective inhbitor of the receptor tyrosine kinase EphB4 (ED50 = 25 nM). NVP-BHG712 blocks Ephrin receptor autophosphorylation and VEGF-induced angiogenesis.
in vivo
NVP-BHG712 (3, 10 and 30 mg/kg, p.o., daily) inhibits VEGF driven tissue growth and angiogenesis[2].
| Animal Model: | Mice arrying chambers[1]. |
| 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. |
References
[1]. martiny-baron, g., et al., the small molecule specific ephb4 kinase inhibitor nvp-bhg712 inhibits vegf driven angiogenesis. angiogenesis, 2010. 13(3): p. 259-67.
[2]. kathawala, r.j., et al., the small molecule tyrosine kinase inhibitor nvp-bhg712 antagonizes abcc10-mediated paclitaxel resistance: a preclinical and pharmacokinetic study. oncotarget, 2015. 6(1): p. 510-21.
[3]. becerikli, m., et al., ephb4 tyrosine-kinase receptor expression and biological significance in soft tissue sarcoma. int j cancer, 2015. 136(8): p. 1781-91.
