General description

A cell-permeable imidazopyridazine compound that acts as a potent, reversible and ATP-competitive inhibitor of Pim-1,2,3, Flt-3 and haspin kinase activities (IC₅₀ = 7, 363, 69, 44 and 34 nM, respectively) with moderate (40% inhibition at 1 µM for c-kit) to excellent selectivity over CDKs, Aurora, Chk1, IKK, JNK, Abl, Raf, PKA, PKC and PI 3-K among 300-kinases. Shown to inhibit RNA synthesis, block phosphorylation of c-Myc-Ser⁶² and STAT3-Tyr⁷⁰⁵, and decrease c-Myc and Mcl-1 protein levels; cause cell cycle arrest and induce apoptosis in CLL lymphocytes and in AML cells, and efficiently arrest the growth of several prostate cancer cells (IC₅₀﹤10 µM).

Legal Information

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

Other Notes

Chen, L.S., et al. 2011. Blood118, 693.Chang, M., et al. 2010. Mol. Cancer Ther.9, 2478.Mumenthaler, S.M., et al. 2009. Mol. Cancer Ther.8, 2882.Chen, L.S., et al. 2009. Blood 114, 4150.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstituion, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)