NVP-BHG712 Chemical Properties

Density 

1.41

storage temp. 

-20°C

solubility 

DMSO: >15mg/mL

form 

powder

pka

13.20±0.70(Predicted)

color 

white to beige

Safety Information

Hazard Codes 

T

Risk Statements 

25

Safety Statements 

45

RIDADR 

UN 2811 6.1 / PGIII

WGK Germany 

3

HS Code 

2933.59.7000

NVP-BHG712 Usage And Synthesis

Uses

NVP-BHG712 is a small molecule specific EphB4, VEGFR2, c-raf, c-src and c-Abl kinase inhibitor with ED50 of 25 nM, 4.2, 0.4, 1.3 and 1.7μM, respectively.

Uses

NVP-BHG712 can be used in biological study and therapeutic use of combinations of kinase inhibitors for treating colorectal cancer.

Definition

ChEBI: 4-methyl-3-[[1-methyl-6-(3-pyridinyl)-4-pyrazolo[3,4-d]pyrimidinyl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide is a member of benzamides.

Biochem/physiol Actions

NVP-BHG712 is a very potent, selective inhbitor of the receptor tyrosine kinase EphB4 (ED50 = 25 nM). NVP-BHG712 blocks Ephrin receptor autophosphorylation and VEGF-induced angiogenesis.

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.

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