676503
VEGFR/Tie-2/PDGFR Tyrosine Kinase Inhibitor
The VEGFR/Tie-2/PDGFR Tyrosine Kinase Inhibitor controls the biological activity of VEGFR/Tie-2/PDGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
VEGFR/Tie-2/PDGFR Tyrosine Kinase Inhibitor, 1-(2-Fluoro-4-((5-methyl-5H-pyrrolo[3,2-d]pyrimidin-4-yl)oxy)phenyl)-3-(3-(trifluoromethyl)phenyl)urea, PDGFR Tyrosine Kinase Inhibitor XXI, VEGFR Tyrosine Kinase Inhibitor XXXIV, VEGFR2 Kinase Inhibitor XXXII, VEGFR1 Kinase Inhibitor VII
SMILES string
O=C(NC1=CC(C(F)(F)F)=CC=C1)NC2=CC=C(OC3=NC=NC4=C3N(C)C=C4)C=C2F
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
light beige
solubility
DMSO: 100 mg/mL
shipped in
ambient
Quality Level
General description
An orally bioavailable pyrrolopyrimidinylurea compound that simultaneously binds to both the adenine and the adjacent hydrophobic pocket of the inactive form of VEGFR2 with high-affinity (type-II inhibitor) and acts as a pseudo-irreversible inhibitor with prolonged action. Shown to potently inhibit the activities of VEGFR2, VEGFR1, Tie-2, PDGFRα, PDGFRβ and c-kit (IC50 = 6.2, 15, 20, 35, 96 and 170 nM, respectively) with moderate to excellent selectivity over B-raf and Aurora-A (IC50 = 0.9 and 1.05 µM) and FGFR1, HER2, EGFR, IR, PKCθ (>10 µM) among 18-kinases. Arrests VEGF-induced HUVECs proliferation (IC50 = 4.4 µM) and suppresses DU145 carcinoma growth in a xenograft nude mouse model (6 mg/kg, b.i.d.).
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 monthst at -20°C.
Other Notes
Oguro, Y., et al. 2010. Bioorg. Med. Chem.18, 7150.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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