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NVP-BHG712 Ephrin receptor inhibitor

Name: NVP-BHG712
Brand: Selleck Chemicals
SKU: S2202
Availability: InStock
Rating: 5 (17 reviews)

Cat.No.S2202

NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; this compound 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.

Chemical Structure

Molecular Weight: 503.48

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.92%

99.92

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src FLT3 HER2 c-Kit Bcr-Abl MEK BTK IGF-1R ALK Syk Trk receptor Axl CSF-1R c-RET FAK Mertk Tie-2 DYRK Tyro3 ROS1 Pyk2 RON DDR ACK Fer kinase
Related Products	Ehp-inhibitor-1 EphA2 Antibody [A19C20] Phospho-EphA2 (Ser897) Antibody [G4G3] NVP-BHG712 isomer Ifabotuzumab (Anti-EphA3) AWL-II-38.3 Anti-EphA2 (MEDI-547) EphB4 Antibody [C23G10] Phospho-EphA2 (Tyr588) Antibody [F13K2] ALW II-41-27

Chemical Information, Storage & Stability

Molecular Weight	503.48	Formula	C₂₆H₂₀F₃N₇O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	940310-85-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)NC3=C4C=NN(C4=NC(=N3)C5=CN=CC=C5)C

Solubility

In vitro
Batch:

DMSO : 101 mg/mL (200.6 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.8mg/ml (1.59mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.8mg/ml (1.59mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	NMP 1 PEG 300 (10 2 90, v 3 v) Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (19.86mM)	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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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.

Mechanism of Action

Features	Discriminates between VEGFR and EphB4.
Targets/IC₅₀/Ki	EphB4 ^[1] (cell based assays ) 25 nM(ED50) C-Raf ^[1] (Cell-free assay) 0.395 μM c-Src ^[1] (Cell-free assay) 1.266 μM c-Abl ^[1] (Cell-free assay) 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, this compound (10 mg/kg/kg, p.o.) potently reverses VEGF enhanced tissue formation and vessel growth. It (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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/20803239/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-EphB4 / p-EphB2 / p-EphB3 / p-EphA2 / p-EphA3		20803239

Tech Support

Handling Instructions

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