PDGFR 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 µM, >10 µM, >10 µM, 45.8 µM and >100 µM, respectively).

Cell permeable: yes

Primary Target
PDGFR Tyrosine Kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 4.2 nM and 45 nM for -β and -α form of PDGFR, respectively

Packaged under inert gas

Toxicity: Harmful (C)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Ho, C.Y., et al. 2005. J. Med. Chem.48, 8163.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany