NVP-BHG712EphB4 inhibitor,potent and selective CAS# 940310-85-0 |
- Dasatinib (BMS-354825)
Catalog No.:BCC1281
CAS No.:302962-49-8
- Saracatinib (AZD0530)
Catalog No.:BCC1166
CAS No.:379231-04-6
- Bosutinib (SKI-606)
Catalog No.:BCC1167
CAS No.:380843-75-4
- Dasatinib hydrochloride
Catalog No.:BCC1517
CAS No.:854001-07-3
- A-770041
Catalog No.:BCC1323
CAS No.:869748-10-7
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 940310-85-0 | SDF | Download SDF |
| PubChem ID | 16747388 | Appearance | Powder |
| Formula | C26H20F3N7O | M.Wt | 503.48 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 31.25 mg/mL (62.07 mM; Need ultrasonic) | ||
| Chemical Name | 4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | ||
| 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 | ||
| Standard InChIKey | ZCCPLJOKGAACRT-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C26H20F3N7O/c1-15-8-9-16(25(37)32-19-7-3-6-18(12-19)26(27,28)29)11-21(15)33-23-20-14-31-36(2)24(20)35-22(34-23)17-5-4-10-30-13-17/h3-14H,1-2H3,(H,32,37)(H,33,34,35) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective inhibitor of EphB4 kinase; exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3. Inhibits EphB4 autophosphorylation in transiently transfected HEK 293 cells. Also inhibits VEGF-induced angiogenesis in vivo; thought to inhibit EphB4 forward signaling. Orally active. |
NVP-BHG712 Dilution Calculator
NVP-BHG712 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.9862 mL | 9.9309 mL | 19.8618 mL | 39.7235 mL | 49.6544 mL |
| 5 mM | 0.3972 mL | 1.9862 mL | 3.9724 mL | 7.9447 mL | 9.9309 mL |
| 10 mM | 0.1986 mL | 0.9931 mL | 1.9862 mL | 3.9724 mL | 4.9654 mL |
| 50 mM | 0.0397 mL | 0.1986 mL | 0.3972 mL | 0.7945 mL | 0.9931 mL |
| 100 mM | 0.0199 mL | 0.0993 mL | 0.1986 mL | 0.3972 mL | 0.4965 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
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.
