Shelf life (days): 1460.0
Formulation: A solid
Formal Name: N-[4-(4-aminofuro[2,3-d]pyrimidin-5-yl)phenyl]-N'-[2-fluoro-5-(trifluoromethyl)phenyl]-urea
Purity: ≥98%
Formula Markup: C20H13F4N5O2
Formula Weight: 431.343332
CAS Number: 501693-48-7
Notes: A Tie2 and VEGFR inhibitor (IC50s = 13.49 and 7.76 nM, respectively); selective for Tie2 and VEGFR2 over Akt3, Cdk2, EGFR, and GSK3 (IC50s = >10,000, >10,000, 10,000, and 2,187 nM, respectively) but does inhibit VEGFR1 and VEGFR3 (IC50s = 8.51 and 7.59 nM, respectively); inhibits VEGF-induced increases in the proliferation of HUVECs and GM-CSF-induced increases in Tie2 autophosphorylation in NIH3T3 fibroblasts expressing chimeric FMS and Tie2 receptors (IC50s = 2.6 and 18.3 nM, respectively); reduces tumor volume and intratumoral vessel density in an HT-29 colon cancer mouse xenograft model at 3, 10, or 30 mg/kg per day; prevents decreases in body temperature in a mouse model of Tnf-α-induced lethal shock at 20 mg/kg
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