FGFR-IN-23

FGFR-IN-23 (Compound 9p) is a covalent pan FGFR inhibitor with IC50s of 14, 4.2, 5 and 220 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. FGFR-IN-23 also has potent inhibitory activity against gatekeeper mutants, such as FGFR1V561M and FGFR3V555M. FGFR-IN-23 suppresses the activation of FGFR-mediated signaling and induces apoptosis. FGFR-IN-23 shows significant antitumor efficacy in RT112 xenograft mouse models. FGFR-IN-23 can be used for cancers and its drug resistance research[1].

Product Specifications

UNSPSC

12352005

Target

Akt; Apoptosis; ERK; FGFR; p38 MAPK

Related Pathways

Apoptosis; MAPK/ERK Pathway; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Field of Research

Cancer

Smiles

C=CC(NC1=CC2=C(C=C1)C(C3=CNC4=NC=C(C5=CN(CCN6CCOCC6)N=C5)N=C43)=CN2C)=O

Molecular Formula

C27H28N8O2

Molecular Weight

496.56

References & Citations

[1]Deng W, et al. Design, Synthesis and Biological Evaluation of 7- (1-Methyl-1H-indole-3-yl) -5H-pyrrolo[2,3-b]pyrazine Derivatives as Novel Covalent pan-FGFR Inhibitors to Overcome Clinical Resistance. J Med Chem. 2025 Sep 25;68 (18) :19415-19437.