fgfr-4-in-1

FGFR4-IN-1 is a potent FGFR4 inhibitor (IC50: 0.7 nM).

FGFR4-IN-16 (CY-15-2) is a covalent inhibitor of FGFR-4, employed in cancer research [1].

FGFR4-IN-18 (compound 8z) is an inhibitor of FGFR4, useful for cancer research.

FGFR4-IN-19 (compound 8B) is a potent covalent inhibitor of fibroblast growth factor receptor 4 (FGFR4) with an IC50 value of 1.2 nM. It achieves high efficiency and selectivity by covalently targeting the rare cysteine (C552) in the FGFR4 kinase domain. FGFR4-IN-19 is applicable for hepatocellular carcinoma (HCC) research.

FGFR4-IN-10 (compound 5a) is a selective and potent FGFR4 inhibitor (IC50: 70.7 nM) and does not inhibit other FGFR family members (i.e., FGFR1, FGFR2, and FGFR3).

FGFR4-IN-11 is a selective, potent, covalently bound FGFR4 inhibitor (IC50: 2.1 nM). FGFR4-IN-11 significantly inhibits the FGF19/FGFR4 signaling pathway and exhibits anticancer effects.

FGFR4-IN-14 (Compound 27i) is a selective FGFR4 inhibitor with an IC50 of 2.4 nM, effectively inhibiting cell proliferation in V550L and N535K mutant strains. It shows IC50 values of 21 nM against Huh7 cells, 2.5 nM against BaF3/ETV6-FGFR4-V550L cells, and 171 nM against BaF3/ETV6-FGFR4-N535K cells. FGFR4-IN-14 demonstrates significant antitumor efficacy in the Huh7 xenograft model and is utilized in hepatocellular carcinoma (HCC) research [1].

FGFR4-IN-17 (Compound (S)-23), a piperazinyl diflurindan derivative featuring a pyridinyl group, functions as an inhibitor of FGFR. It exhibits IC 50 values of 24.2 nM for FGFR1, 16.1 nM for FGFR2, 78.0 nM for FGFR3, and 68.0 nM for FGFR4. Notably, FGFR4-IN-17 demonstrates significant antitumor activity [1].

FGFRs-IN-1 (Compound A16) is an orally active inhibitor targeting FGFR1/2/3/4, with IC50 values of 2.3, 7, 11, and 163 nM respectively. It also inhibits VEGFR1/2/3, Abl, and Flt3, with IC50 values of 61, 176, 112, 26, and 353 nM. The compound shows weak inhibition of CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and it inhibits epithelial-mesenchymal transition (EMT) in A549 cells stimulated by TGF-β1. Additionally, FGFRs-IN-1 demonstrates anti-inflammatory activity in mouse models of lung fibrosis induced by Bleomycin and liver fibrosis induced by CCl4.

Arg-IN-1 is a selective covalent inhibitor targeting Arginine (Arg), with IC50 values of 9.7 nM and 30.4 nM for FGFR2 and FGFR3, respectively. This compound is designed to potentially avoid the off-target toxicity of FGFR1/4 and overcome acquired resistance, offering potential in cancer therapies targeting FGFR.

ODM-203 sodium is an orally available, selective, and efficient FGFR and VEGFR inhibitor, with antitumor activity, inhibiting FGFR3/1/2 and VEGFR3/2/1/4, inducing antitumor immunity, useful in solid tumor research.