NVP-BHG712

Catalog No.S2202 Batch:S220203

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Technical Data

Formula

C26H20F3N7O
Molecular Weight 503.48 CAS No. 940310-85-0
Solubility (25°C)* In vitro DMSO 101 mg/mL (200.6 mM)
Ethanol 3 mg/mL (5.95 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
NMP PEG 300 (10 90, v v)
10.0mg/ml Taking the 1 mL working solution as an example, add 10 mg of this product to 1 ml of 1 ml NMP+PEG 300 (10+90, v+v) clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

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
EphB4 [1]
(cell based assays )		 C-Raf [1]
(Cell-free assay)		 c-Src [1]
(Cell-free assay)		 c-Abl [1]
(Cell-free assay)
25 nM(ED50) 0.395 μM 1.266 μM 1.667 μM
In vitro NVP-BHG712 treatment also dose dependently leads to the inhibition of RTK autophosphorylation in stable transfected A375 melanoma cells with EC50 of 25 nM and 4.2 μM for EphB4 and VEGFR2, respectively. [1]
In vivo In a growth factor-induced angiogenesis model, NVP-BHG712 (3 mg/kg, p.o) significantly suppresses VEGF stimulated tissue formation and vascularization by inhibiting EphB4 forward signaling. Furthermore, NVP-BHG712 (10 mg/kg/kg, p.o.) potently reverses VEGF enhanced tissue formation and vessel growth. NVP-BHG712 (3 mg/kg, p.o.) shows a long lasting exposure with concentrations around 10 μM in plasma as well as in lung and liver tissue for up to 8 hours, and thus results in a long lasting inhibition of EphB4 kinase activity in mice. [1]
Features Discriminates between VEGFR and EphB4.

Protocol (from reference)

Animal Study:[1]
  • Animal Models

    VEGF-mediated angiogenesis in vivo is induced in a growth factor implant model in mice.

  • Dosages

    ≤30 mg/kg

  • Administration

    Administered via p.o.

Customer Product Validation

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Selleck's NVP-BHG712 has been cited by 12 publications

EGFR-phosphorylated GDH1 harmonizes with RSK2 to drive CREB activation and tumor metastasis in EGFR-activated lung cancer [ Cell Rep, 2022, 41(11):111827] PubMed: 36516759
Adaptive activation of EFNB2/EPHB4 axis promotes post-metastatic growth of colorectal cancer liver metastases by LDLR-mediated cholesterol uptake [ Oncogene, 2022, 10.1038/s41388-022-02519-z] PubMed: 36376513
Antiviral drug screen identifies DNA-damage response inhibitor as potent blocker of SARS-CoV-2 replication [ Cell Rep, 2021, 35(1):108940] PubMed: 33784499
EFNA4 promotes cell proliferation and tumor metastasis in hepatocellular carcinoma through a PIK3R2/GSK3β/β-catenin positive feedback loop [ Mol Ther Nucleic Acids, 2021, 25:328-341] PubMed: 34484860
Targeting the EphB4 receptor tyrosine kinase sensitizes HER2-positive breast cancer cells to Lapatinib. [ Cancer Lett, 2020, 475:53-64] PubMed: 32006616
Identification of SYK Inhibitor, R406 as a Novel Senolytic Agent [ Aging (Albany NY), 2020, 7;12(9):8221-8240] PubMed: 32379705
EPHB4 inhibition activates ER stress to promote immunogenic cell death of prostate cancer cells. [ Cell Death Dis, 2019, 10(11):801] PubMed: 31641103
Deep Learning Enhancing Kinome-Wide Polypharmacology Profiling: Model Construction and Experiment Validation. [ J Med Chem, 2019, 10.1021/acs.jmedchem.9b00855] PubMed: 31364850
Mitochondrial metabolic reprograming via BRAF inhibition ameliorates senescence. [ Exp Gerontol, 2019, 126:110691] PubMed: 31421186
Comparative analysis of the phototoxicity induced by BRAF inhibitors and alleviation through antioxidants. [ Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520] PubMed: 31618797

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.