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]

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

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

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.

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

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

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

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-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).

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.

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

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

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.

EGFR-IN-16 (AG473) is an inhibitor of EGFR in human A431 cells.

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.

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].

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].

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].

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).

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.