FGFR3-IN-1

FGFR3-IN-1 (compound 1) is a fibroblast growth factor receptor (FGFR) inhibitor that targets FGFR1 (IC50: 40 nM), FGFR2 (IC50: 5.1 nM), and FGFR3 (IC50: 12 nM).

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.

BW710 is an orally active inhibitor specifically targeting fibroblast growth factor receptor 2 (FGFR2). It effectively inhibits the proliferation of BaF3-FGFR2 cells with an IC50 value of 2.8 nM. BW710 completely suppresses FGFR2 enzymatic activity and demonstrates selectivity among 75 tyrosine kinases, including FGFR1, FGFR3, and FGFR4, at a 1 μM concentration. Additionally, BW710 impedes FGFR2 signaling and selectively inhibits the proliferation of cancer cells driven by FGFR2. It exhibits promising pharmacokinetic properties, with an oral bioavailability of 29% in mice.

FGFR2 3-IN-2 (compound 10) is an orally active inhibitor targeting FGFR2 and FGFR3. It exhibits IC50 values of 3.7 nM for FGFR2 and 31.2 nM for FGFR3, with a pre-incubation time of 1 hour. FGFR2 3-IN-2 demonstrates selectivity over FGFR1 4 and other kinases, and does not cause diarrhea or increased serum phosphate in vivo. In the SNU-16 gastric cancer model, FGFR2 3-IN-2 can induce tumor stasis or regression.

FGFR-IN-1 is a highly effective inhibitor targeting the Fibroblast Growth Factor Receptor (FGFR) group, comprising FGFR1, FGFR2, and FGFR3, with an impressive inhibitory concentration (IC 50) of less than 100 nM (US20130338134A1, example 219).

FGFR2-IN-1 is an FGFR inhibitor that inhibits FGFR1, FGFR2, and FGFR3 with IC50s of 460, 140, and 2200 nM, respectively.FGFR2-IN-1 can be used for the study of cancers associated with FGFR2.13460-73-81-1

FGFR-IN-2 (compound 1) is a potent FGFR inhibitor, targeting FGFR1 (IC50: 7.3 nM), FGFR2 (IC50: 4.3 nM), FGFR3 (IC50: 7.6 nM), and FGFR4 (IC50: 11 nM).

Roridin E inhibits the receptor tyrosine kinases FGFR3, IGF-1R, PDGFRβ, and TrkB (IC50s = 0.4, 0.4, 1.4, and 1 μM, respectively) and induces cytotoxicity in multiple breast cancer cell lines (IC50s = 0.02-0.05 nM). It also inhibits proliferation in a panel of additional cancer cell lines (IC50s = <0.01 μM).

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.

Vosoritide (BMN 111), a modified recombinant C-type natriuretic peptide (CNP) analogue, engages with natriuretic peptide receptor type B (NPR-B) to diminish the function of fibroblast growth factor receptor 3 (FGFR3). This compound is employed in the study of achondroplasia and dwarfism [1] [2] [3].

FGFR-IN-11 (compound I-5) is an orally active, covalent inhibitor of FGFR, with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4). This compound demonstrates nanomolar potency in inhibiting the proliferation of various cancer cells and significantly hinders tumor growth in xenograft mouse models [1].

FGFR3-IN-7 is a potent, selective inhibitor of FGFR 3, demonstrating an IC50 value of less than 350 nM , and is utilized in cancer research [1].

FGFR3-IN-6 is a potent, selective inhibitor of FGFR 3, exhibiting an IC50 value of less than 350 nM , and is utilized in cancer research [1].

FGFR3-IN-9 (example27) functions as a selective FGFR3 inhibitor [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].