A cell-permeable symmetrical indolylmethanone kinase inhibitor that is more selective toward Flt3 over PDGFR either in cell-based receptor autophosphorylation (IC₅₀ = 40 nM vs. 300 nM) or in cell-free kinase reactions (IC₅₀ = 33 nM vs. 171 nM) and potently induces apoptosis in Flt3-expressing primary AML patient blasts. Affects Abl- or Kit-dependent cell growth only at much higher concentrations (IC₅₀ = 4.2 and ≥0.5 µM, respectively), while exhibiting little effect against IL-3-mediated cellular signaling. The molecular mechanism of inhibition is presumably due to interaction at the enzyme′s ATP-binding site.

Cell permeable: yes

Primary Target
Flt-3

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 40 nM against Flt3 in cell-based receptor autophosphorylation; 33 nM against Flt3 in cell-free kinase reactions

Packaged under inert gas

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

Mahboobi, S., et al. 2006. J. Med. Chem.49, 3101.

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

Toxicity: Irritant (B)