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Background Information:
NVP-BHG712 is an orally bioavailable selective inhibitor of EphB4 kinase with IC50 of 25 nM in cellular assays; Displaying selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3. It inhibits EphB4 autophosphorylation in transiently transfected HEK 293 cells. It also inhibits VEGF-induced angiogenesis in vivo thought to inhibit EphB4 forward signaling which appears to be an important mediator of VEGF induced angiogenesis (ref 1).
Reference:
1. Martiny-Baron G, et al. The small molecule specific EphB4 kinase inhibitor NVP-BHG712 inhibits VEGF driven angiogenesis. Angiogenesis. 2010 Sep;13(3):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.
APIM050209: NVP-BHG712 (BHG-712)
CAS No.: 940310-85-0.
Molecular Formula: C26H20F3N7O.
Molecular Weight: 503.5 (or refer to Certificate of Analysis, batch-specific).
Purity: 99.5% by HPLC at 214 and 254 nm.
QC: HPLC, H-NMR and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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