CQ1373

CQ1373 is a potent RET inhibitor, demonstrating cellular potency with IC50 values of 13.0, 25.7 and 28.4 nM against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C and CCDC6-RET-G810R, respectively. CQ1373 exhibits good selectivity toward wild-type RET and solvent front mutants G810C/R with IC50 values of 4.2, 7.1 and 32.4 nM, respectively. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. CQ1373 induces Apoptosis and cell cycle arrest in BaF3 cells. CQ1373 exhibits anti-tumor efficacy and can be used for cancer research[1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; RET

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

CC(C)(C(F)(F)F)C1=CC(NC(NC2=C(Cl)C=C(/C=C/C3=C(C4=CN=CC(OC)=C4)C=NN3)C=C2)=O)=NO1

Molecular Formula

C25H22ClF3N6O3

Molecular Weight

546.93

References & Citations

[1]Xu M, et al. Design, synthesis and evaluation of (E) -1- (4- (2- (1H-pyrazol-5-yl) vinyl) phenyl) derivatives as next generation selective RET inhibitors overcoming RET solvent front mutations (G810C/R) . Eur J Med Chem. 2025 Mar 15;286:117294.