NVP-BHG712 |
| Catalog No.GC14332 |
NVP-BHG712는 EphA2 및 EphB4에 대해 IC50 값이 각각 3.3nM 및 3.0nM인 경구 활성 EphB4 키나제 자가인산화 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 940310-85-0
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
|
Cell lines |
Hek293 cells transfected with different EphRs |
|
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. |
|
Reacting condition |
10 ~ 1000 nM; 1 hr |
|
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]: | |
|
Animal models |
Mice carrying chambers containing VEGF |
|
Dosage form |
3, 10 and 30 mg/kg/d; p.o. |
|
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. |
|
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. |
|
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. | |
| Cas No. | 940310-85-0 | SDF | |
| Chemical Name | 4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | ||
| 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 | ||
| Formula | C26H20F3N7O | M.Wt | 503.48 |
| Solubility | ≥ 25.15mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9862 mL | 9.9309 mL | 19.8618 mL |
| 5 mM | 0.3972 mL | 1.9862 mL | 3.9724 mL |
| 10 mM | 0.1986 mL | 0.9931 mL | 1.9862 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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