85-2077-37　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, VEGFR Tyrosine Kinase Inhibitor XXXIV, VEGFR2 Kinase Inhibitor XXXII, VEGFR1 Kinase Inhibitor VII, PDGFR Tyrosine Kinase Inhibitor XXI) 5mg　217867

特徴

• 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, PDGFRa, PDGFRb and c-kit (IC50=6.2, 15, 20, 35, 96 and 170nM, respectively) with moderate to excellent selectivity over B-raf and Aurora-A (IC50=0.9 and 1.05uM) and FGFR1, HER2, EGFR, IR, PKCth (>10uM) among 18-kinases. Arrests VEGF-induced HUVECs proliferation (IC50=4.4uM) and suppresses DU145 carcinoma growth in a xenograft nude mouse model (6mg/kg, b.i.d.).
• Formula:C21H15F4N5O2
• Molecular Weight:445.4
• Solubility:DMSO (100mg/ml)
• Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.