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217867 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) CAS:

Specifications
Grade
Highly Purified
Molecular Formula
C21H15F4N5O2
Molecular Weight
445.4
EU Commodity Code
38220090
Shipping Temp
Blue Ice
Storage Temp
-20°C

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.
Purity
~95% (HPLC)
Concentration
Not determined
Form
Supplied as a light beige solid.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
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