| Identification | Back Directory | [Name]
5-((7-(BENZYLOXY)QUINAZOLIN-4-YL)AMINO)-4-FLUORO-2-METHYLPHENOL | [CAS]
193001-14-8 | [Synonyms]
CS-744
ZM323881
KDR/FLK-1 INHIBITOR V
VEGF RECEPTOR 2 KINASE INHIBITOR V
5-((7-(BENZYLOXY)QUINAZOLIN-4-YL)AMINO)-4-FLUORO-2-METHYLPHENOL
4-Fluoro-2-methyl-5-[[7-(phenylmethoxy)-4-quinazolinyl]amino]phenol
Phenol, 4-fluoro-2-methyl-5-[[7-(phenylmethoxy)-4-quinazolinyl]amino]- | [Molecular Formula]
C22H18FN3O2 | [MDL Number]
MFCD09037564 | [MOL File]
193001-14-8.mol | [Molecular Weight]
375.4 |
| Chemical Properties | Back Directory | [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 | [form ]
White to off-white solid. | [pka]
9.99±0.23(Predicted) |
| Hazard Information | Back Directory | [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]. | [target]
VEGFR-2/KDR | [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. |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
|