PDGF Receptor Tyrosine Kinase Inhibitor IV

A cell-permeable indenopyrazole compound that displays potent antiproliferative properties in several human tumor cell lines (IC50 <33 nM). Shown to act as an ATP-competitive and reversible inhibitor of PDGFR (IC50 = 4.2 nM and 45 nM for -β and -α , respectively) and c-Abl (IC50 = 22 nM). Exhibits less activity towards Lck, c-Src, and Fyn (IC50 = 100 nM, 185 nM and 378 nM, respectively) and exhibits little or no inhibition toward VEGFR, HER-2, Cdk's-1, -2, -4 &-7, bFGFR-1 and EGFR (IC50 = 3.1 µ M, >10 µ M, >10 µ M, 45.8 µ M and >100 µ M, respectively).

627518-40-5

C₁₈H₁₆FN₃O₂

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