5-((7-(BENZYLOXY)QUINAZOLIN-4-YL)AMINO)-4-FLUORO-2-METHYLPHENOL
- CAS NO.:193001-14-8
- Empirical Formula: C22H18FN3O2
- Molecular Weight: 375.4
- MDL number: MFCD08703130
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-10-28 16:48:35
What is 5-((7-(BENZYLOXY)QUINAZOLIN-4-YL)AMINO)-4-FLUORO-2-METHYLPHENOL?
Definition
ChEBI: ZM 323881 is a member of the class of quinazolines carrying 2-fluoro-4-methyl-5-hydroxyanilino and benzyloxy substituents at positions 4 and 7 respectively. It has a role as a vascular endothelial growth factor receptor antagonist. It is a benzyl ether, an aromatic ether, a member of quinazolines, a secondary amino compound, a substituted aniline, a halophenol, a member of monofluorobenzenes, an organic cation and a fluorophenol. It is a conjugate base of a ZM 323881(1+).
Biological Activity
zm323881 inhibits vegf-a-induced endothelial cell proliferation (ic50 = 8 nm) and vegf-r2 tyrosine phosphorylation (ic50 < 2 nm).vascular endothelial growth factor (vegf) increases vascular permeability and angiogenesis in many pathological conditions, such as cancer, arthritis, and diabetes. vegf activates vegf-receptor 1 (vegf-r1) and vegf-receptor 2 (vegf-r2) that autophosphorylate to initiate a signaling cascade resulting in angiogenesis and increased microvascular permeability. zm323881 is a potent and selective inhibitor of vegf-r2 tyrosine kinase.
in vitro
zm323881 was found to inhibit vegf-a-induced endothelial cell proliferation (ic50 = 8 nm) and vegf-r2 tyrosine phosphorylation in vitro (ic50 < 2 nm) [1].
in vivo
vegf-amediated increases in vascular permeability in perfused mesenteric microvessels in vivo were reversibly abolished by both zm323881 and the class iii receptor tyrosine kinase inhibitor ptk787/zk222584, suggesting that vegf-r2 phosphorylation is necessary for vegf-a-mediated increases in microvascular permeability in vivo [1].
References
[1] whittles ce, pocock tm, wedge sr, kendrew j, hennequin lf, harper sj, bates do. zm323881, a novel inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity. microcirculation. 2002;9(6):513-22.
Properties of 5-((7-(BENZYLOXY)QUINAZOLIN-4-YL)AMINO)-4-FLUORO-2-METHYLPHENOL
Boiling point: | 543.6±50.0 °C(Predicted) |
Density | 1.342±0.06 g/cm3(Predicted) |
storage temp. | Store at -20°C |
solubility | Soluble in DMSO |
pka | 9.99±0.23(Predicted) |
form | White to off-white solid. |
Safety information for 5-((7-(BENZYLOXY)QUINAZOLIN-4-YL)AMINO)-4-FLUORO-2-METHYLPHENOL
Computed Descriptors for 5-((7-(BENZYLOXY)QUINAZOLIN-4-YL)AMINO)-4-FLUORO-2-METHYLPHENOL
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