FGFR-IN-1

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).

Futibatinib (TAS-120) is an orally active, potent, selective, highly bioavailable, and irreversible FGFR inhibitor with IC50 values ​​of 3.9, 1.3, 1.6, and 8.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. [2]

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.

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].

FGFR-IN-12 (example 14) is a potent FGFR inhibitor that belongs to the class of pyrimidinyl aryl urea derivatives [1].

FGFR-IN-13 (compound III-30), an irreversible covalent inhibitor of the fibroblast growth factor receptor (FGFR), effectively modulates signaling through FGFR1 (IC 50 = 0.20 ± 0.02 nM) and FGFR4 (IC 50 = 0.40 ± 0.03 nM). It suppresses the expression of crucial proteins such as total-PARP and Bcl-2, while enhancing the expression of Cleaved-PARP and Bax in a dose-dependent manner. Notably, FGFR-IN-13 demonstrates considerable antitumor and oral activity [1].

FGFR-IN-16 (compound 7N) is a potent inhibitor of FGFR1, FGFR2, and FGFR4, exhibiting IC50 values of 8 nM, 4 nM, and 3.8 nM respectively. It plays a crucial role in cancer research.

FGFR-IN-15 (compound 18i) acts as a pan-FGFR inhibitor, exhibiting potent inhibitory activity against FGFR1-4.

FGFR-IN-17 (Compound 12l) is an orally active irreversible inhibitor of FGFR, effectively suppressing both FGFR and its mutants. It inhibits the proliferation and migration of non-small cell lung cancer cells and induces apoptosis. FGFR-IN-17 demonstrates anti-tumor activity.

FGFR-IN-18 (Compound KF7) is a covalent inhibitor targeting lysine on FGFR, exhibiting IC50 values of 1.1 nM for FGFR2, 1.3 nM for FGFR1, and 31.5 nM for FGFR4. It also shows affinity for FGFR3, with an inhibition rate of 52% at 10 nM. FGFR-IN-18 covalently modifies Lys485, a reactive site on FGFR.

JK-P3 is a pyrazole-based inhibitor of VEGFR-2 (IC50: 7.8 μM). JK-P3 inhibits FGFR 1 3 kinase activity in vitro, but has no effect on FGFR signaling in cell-based assays. The compound blocks wound healing and tube formation in HUVEC without effecting endo

PD153035 (NSC-669364) hydrochloride is an effective and selective inhibitor of EGFR (Ki IC50: 5.2 29 pM, in cell-free assays); little inhibitory against FGFR, PGDFR, InsR, CSF-1 and Src.

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.

Antifibrotic agent 1 is an orally active medication designed to treat idiopathic pulmonary fibrosis (IPF). It effectively mitigates IPF-related processes, including TGF-β-induced epithelial-mesenchymal transition (EMT) and fibroblast-to-myofibroblast transition (FMT), as well as profibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α, and Src family kinases (SFKs), while sparing VEGFR, FGFR, and Abl to minimize off-target toxicity. In a bleomycin (BLM)-induced pulmonary fibrosis mouse model, it demonstrates strong antifibrotic activity.

Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor that acts on KDR, Flt-1, FGFR1, and PDGFRα with IC50 values of 4 nM, 20 nM, 4 nM, and 2 nM, respectively.

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-7 (compound 17) is an orally active, potent FGFR modulator that penetrates the blood-brain barrier, exhibits neuroprotective properties, enhances brain exposure, and decreases the likelihood of phospholidosis, proving valuable for research on neurodegenerative diseases [1].

FGFR-IN-3 (compound 6) is a highly potent, orally active modulator of FGFR (fibroblast growth factor receptor) with the ability to penetrate the blood-brain barrier (BBB). It exhibits significant neuroprotective properties, making it a promising candidate for research on neurodegenerative diseases [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).

Multi-kinase-IN-2 is an orally active inhibitor of angiokinases. multi-kinase-IN-2 significantly inhibits the activity of angiokinases such as VEGFR-1 2 3, PDGFRα β, FGFR-1, LYN and c-KIT kinases. -IN-2 significantly attenuates phosphorylation of AKT and ERK proteins, induces apoptosis and has anticancer effects.

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).

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.

ALK2-IN-5, a pyrazolopyrimidine compound, serves as an inhibitor of ALK2 and FGFR, targeting disorders linked with their activity, including cancer [1].

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