PDGFRα kinase inhibitor 3 

PDGFRα kinase inhibitor 3 (Compound L7) is a highly potent inhibitor targeting the PDGFRα^D842V kinase with IC₅₀s values of 23.8 nM and 2.1 nM in biochemical and cellular assays, respectively. PDGFRα kinase inhibitor 3 binds to the ATP-binding pocket of PDGFRα^D842V to block its downstream signaling pathways and inhibit kinase activity. PDGFRα kinase inhibitor 3 can be used for gastrointestinal stromal tumors (GISTs) study^[1].

IC50: PDGFRαD842 V/G680R (64.1 nM), PDGFRαD842 V/T674I (27.6 nM)

385.46

C₂₃H₂₃N₅O

C1(N2C=NC3=C2C=C4C=C3)=CC=C5C(C(N6CCC(CC6)NCCO4)=CC=C5)=N1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Liang H, et al. Designing Macrocyclic Kinase Inhibitors Using Macrocycle Scaffold Hopping with Reinforced Learning (Macro-Hop). J Med Chem. 2025 Mar 27;68(6):6698-6717.  [Content Brief]