UNC3133 

UNC3133 is an orally active, limitedly selective MerTK inhibitor with an IC₅₀ of 3.0 nM. UNC3133 inhibits Axl, Tyro3 and Flt3 kinases, with IC₅₀ values of 17 nM, 31 nM and 6.8 nM, respectively. UNC3133 is applicable to the research of inflammatory diseases and cancers^[1].

UNC3133 potently inhibits purified MerTK kinase activity with an IC₅₀ of 3.0 nM, while also inhibiting Axl, Tyro3, and Flt3 kinases with IC₅₀ values of 17 nM, 31 nM, and 6.8 nM, respectively^[1].
UNC3133 inhibits EGF-stimulated MerTK phosphorylation in HEK293 cells expressing an EGFR-MerTK chimeric protein with an EC₅₀ of 110 nM^[1].
UNC3133 (300 nM) demonstrates limited kinome selectivity, with greater than 50% inhibition of 12 kinases when tested at 300 nM, including eight tyrosine kinases and four serine/threonine kinases^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

504.71

C₃₀H₄₄N₆O

2011034-35-6

OC(CCCCCCCN1)CCCCN2C3=NC1=NC=C3C(C4=CC=C(C=C4)CN5CCN(CC5)C)=C2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Wang X, et al. Design and Synthesis of Novel Macrocyclic Mer Tyrosine Kinase Inhibitors. ACS Med Chem Lett. 2016;7(12):1044-1049. Published 2016 Sep 13.  [Content Brief]