Merck, 445835-10MG, Mer RTK Inhibitor, UNC569

General description
An orally bioavailable pyrazolopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of Mer receptor tyrosine kinase (IC₅₀ = 2.9 nM; Ki = 4.3 nM) with ~10-fold greater selectivity over other TAM family kinases (IC₅₀ = 37 and 48 nM for Axl and Tyro3, respectively). Also shown to affect the activities of Flt3, MAPKAPK2, RET and Ret-Y791F at 30 nM by 82%, 92%, 59% and 56% in a 72 kinase panel, and block Mer auto-phosphorylation in human Pre-B leukemia 697 cells with an IC₅₀ of 141 nM. Exhibits desirable pharmacokinetic profile and efficacy in mice.
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable fo rup to 6 months at -20°C.
Other Notes
Liu, J., et al. 2012. ACS Med. Chem. Lett.3, 129.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)