PF-06439015

Non Antibodies

ALK, ROS1, FER, LTK and TrkA/B receptors

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

470, 52

A Potent Inhibitor of TrkA/B and other Receptor Tyrosine Kinases

Centrifuge the vial before adding solvent (10, 000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity

41116134

PF-06439015 is a novel potent inhibitor of receptor tyrosine kinases, highly effective against crizotinib-resistant ALK mutants, inhibiting wild-type and mutant ALK phosphorylation with IC50 of 0.8 nM and 0.2 nM-24 nM, respectively. It is shown to inhibit kinase activity of ROS1, FER, LTK and TrkB with IC50 values of under 10 nM1.

Yes

PF-06439015 is a synthetic compound that acts as a potent inhibitor of receptor tyrosine kinases. It inhibits various tyrosine kinases including ALK, ROS1, FER, LTK and TrkB with IC50 values of less than 10 nM1.Tyrosine kinases are a family of enzymes that acts as important mediators of the signaling cascade leading to cell proliferation, differentiation, migration, metabolism, and programmed cell death. Tyrosine kinases catalyze phosphorylation of select tyrosine residues in target proteins2.