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NVP-BHG712
Catalog No. T6348Cas No. 940310-85-0
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.
NVP-BHG712
Catalog No. T6348Cas No. 940310-85-0
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $31 | In Stock | |
| 2 mg | $44 | In Stock | |
| 5 mg | $72 | In Stock | |
| 10 mg | $113 | In Stock | |
| 25 mg | $223 | In Stock | |
| 50 mg | $413 | In Stock | |
| 100 mg | $618 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $80 | In Stock |
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Purity:97.96%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | 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. |
| Targets&IC50 | EphB4:25 nM, C-Raf:0.395 μM, c-Src:1.266 μM, c-ABL:1.667 μM |
| In vitro | In a vascularization model induced by growth factors, NVP-BHG712 (3 mg/kg, p.o) significantly inhibited tissue formation and vascularization stimulated by VEGF through the suppression of EphB4 forward signaling. Additionally, NVP-BHG712 (10 mg/kg, oral administration) effectively reversed the VEGF-enhanced tissue formation and angiogenesis. NVP-BHG712 (3 mg/kg, orally) exhibited a sustained exposure in mouse plasma as well as lung and liver tissues for up to 8 hours at approximately 10 μM concentration, thereby resulting in long-lasting inhibition of EphB4 kinase activity. |
| In vivo | NVP-BHG712 exhibits dose-dependent inhibition of RTK autophosphorylation in A375 melanoma cells stably transfected, with EC50 values of 25 nM for EphB4 and 4.2 μM for VEGFR2. |
| Molecular Weight | 503.48 |
| Formula | C26H20F3N7O |
| Cas No. | 940310-85-0 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 24.7 mg/mL (40 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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