NVP-BHG712 - 10mM in DMSO , CAS No.940310-85-0

CAS: 940310-85-0 Cat. No.: N408613 Molecular Weight: 503.48 EC Number: 804-395-8

GRADE & PURITY 10mM in DMSO

Synonyms

4-methyl-3-(1-methyl-6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

NVP-BHG712 is a specificEphB4inhibitor withED50of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl withIC50of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
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.

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.
Cell Data

cell lines：WST-1, ANBL-6 cells

Concentrations：

Incubation Time：

Powder Purity:≥97%

Specifications

Synonyms

4-methyl-3-(1-methyl-6-(pyridin-3-yl)-1H-pyrazolo[3, 4-d]pyrimidin-4-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

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.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Names and Identifiers

• Isomeric 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
• WGK Germany: 3
• Molecular Weight: 503.48
• Reaxy-Rn: 12906443
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12906443&ln=

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 48 mg/mL (202.75 mM); Ethanol: 48 mg/mL (202.75 mM); Water: 20 mg/mL (84.48 mM)