| Identification | Back Directory | [Name]
NVP-BHG712 | [CAS]
940310-85-0 | [Synonyms]
CS-475
CS-688
NVP-BHG712
NVP-BHG712 (BHG712)
NVP-BHG712 USP/EP/BP
NVP-BHG 712; NVP BHG 712
4-Methyl-3-(1-methyl-6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)-N-(3-(trifluorome
4-methyl-3-(1-methyl-6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide
4-Methyl-3-[[1-methyl-6-(3-pyridinyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide
Benzamide, 4-methyl-3-[[1-methyl-6-(3-pyridinyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]amino]-N-[3-(trifluoromethyl)phenyl]-
NVP-BHG712
4-Methyl-3-[[1-methyl-6-(3-pyridinyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide | [Molecular Formula]
C26H20F3N7O | [MDL Number]
MFCD20272929 | [MOL File]
940310-85-0.mol | [Molecular Weight]
503.49 |
| Chemical Properties | Back Directory | [density ]
1.41 | [storage temp. ]
?20°C | [solubility ]
DMSO: >15mg/mL | [form ]
powder | [pka]
13.20±0.70(Predicted) | [color ]
white to beige | [InChIKey]
ZCCPLJOKGAACRT-UHFFFAOYSA-N | [SMILES]
Cc1ccc(cc1Nc2nc(nc3n(C)ncc23)-c4cccnc4)C(=O)Nc5cccc(c5)C(F)(F)F |
| Safety Data | Back Directory | [Hazard Codes ]
T | [Risk Statements ]
25 | [Safety Statements ]
45 | [RIDADR ]
UN 2811 6.1 / PGIII | [WGK Germany ]
3 | [HS Code ]
2933.59.7000 | [Storage Class]
6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects | [Hazard Classifications]
Acute Tox. 3 Oral |
| Hazard Information | Back Directory | [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. | [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. | [in vivo]
NVP-BHG712 (3, 10 and 30 mg/kg, p.o., daily) inhibits VEGF driven tissue growth and angiogenesis[2]. | Animal Model: | Mice arrying chambers[1]. | | Dosage: | 3, 10 and 30 mg/kg. | | Administration: | P.O. daily for 4 days. | | Result: | Significantly inhibited VEGF stimulated tissue formation and vascularization at doses of daily 3 mg/kg. Administration of 10 mg/kg/kg p.o. was sufficient to reverse VEGF enhanced tissue formation and vessel growth. |
| [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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