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NVP-BHG712
NVP-BHG712 is a potent inhibitor of EphB4 and VEGFR2 with ED50 value of 25 nM and 4200 nM, respectively [1].
Ephrin type-B receptor 4 (EphB4) is a protein and plays an important role in mediating a variety of developmental processes by working with its ligand. It has been revealed that the over-expression of EphB4 is correlated with several types of tumor [1, 3].
NVP-BHG712 is a potent EphB4 inhibitor and has less inhibition activity on EphB2, EphA2, EphB3 and EphA3. When tested with Hek293 cells transfected different EphRs, administration of NVP-BHG712 inhibited EphRs autophosphorylation in a dose-dependent manner with preference for EphB4, followed by EphB2, EphA2, EphB3 and EphA3 [1]. In HEK293/ABCC 10 cell line, NVP-BHG712 treatment markedly increased cells sensitivity to paclitaxel at the dose of 0.25 μM and 0.5μM [2]. When treated synovial sarcoma cell line with NVP-BHG712, the result showed that it markedly decreased cell proliferation rate and vitality [3].
In VEGF driven angiogenesis tissue model, NVP-BHG712 treatment significantly inhibited VEGF stimulated tissue formation and vascularization by functioning on EphB4 which involved in VEGF driven angiogenesis [1]. In HEK293/ABCC 10 cells subcutaneous xenograft mouse model, co-administration of NVP-BHG712 (25 mg/kg) and paclitaxel (15 mg/kg) markedly decreased tumor volumes, sizes and weights [2]. Using an appropriate sarcoma lung metastasis xenograft model, NVP-BHG712 decreased lung metastasis formation (p?
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.
- 1. Tiancheng Li, Han Wang, et al. "The role of EphB4/ephrinB2 signaling in root repair after orthodontically-induced root resorption." Am J Orthod Dentofacial Orthop. 2021 Mar;159(3):e217-e232. PMID:33487501
- 2. Tiancheng Li, Han Wang, et al. "Intermittent parathyroid hormone promotes cementogenesis via ephrinB2‐EPHB4 forward signaling." J Cell Physiol. 2020 Aug 1. PMID:32740946
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 503.48 |
| Cas No. | 940310-85-0 |
| Formula | C26H20F3N7O |
| Solubility | ≥25.15 mg/mL in DMSO; insoluble in H2O; ≥6.69 mg/mL in EtOH with ultrasonic |
| Chemical Name | 4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)NC3=NC(=NC4=C3C=NN4C)C5=CN=CC=C5 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Hek293 cells transfected with different EphRs |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
10 ~ 1000 nM; 1 hr |
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Applications |
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. |
| Animal experiment [1]: | |
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Animal models |
Mice carrying chambers containing VEGF |
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Dosage form |
3, 10 and 30 mg/kg/d; p.o. |
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Applications |
In VEGF driven angiogenesis tissue model, NVP-BHG712 significantly inhibited VEGF stimulated tissue formation and vascularization at a dose as low as 3 mg/kg/d. At the dose of 10 mg/kg/d, NVP-BHG712 was sufficient to reverse VEGF induced tissue formation and vessel growth. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. |
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| Description | NVP-BHG712 is a specific inhibitor of EphB4 with an ED50 value of 25 nM. | |||||
| Targets | EphB4 | C-Raf | c-Src | c-Abl | Tie-2 | |
| IC50 | 25 nM(ED50) | 0.395 μM | 1.266 μM | 1.667 μM | >10 μM | |
Quality Control & MSDS
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Chemical structure
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