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 (FGFR-IN-1) is a novel, potent and highly selective FGFR inhibitor, used for antitumor treatment.

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

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

FGFR1/VEGFR2-IN-1 (compound 2b) is an inhibitor of both FGFR1 and VEGFR2, applicable in cancer research [1].

FGFR1 inhibitor-6 is a potent inhibitor of FGFR1 (IC50: 16.31 nM) with cytotoxic activity. fGFR1 inhibitor-6 is capable of blocking the cell cycle in pro-G1 and G2/M phases and inducing apoptosis.

FGFR1 inhibitor-10 (Compound 4i), with an IC50 of 28 nM, effectively inhibits FGFR1 phosphorylation. This compound demonstrates anti-angiogenic and anti-invasion properties, as well as a significant anti-tumor effect [1].

FGFR1 Inhibitor 7 (compound 5), a potent FGFR1 tyrosine kinase inhibitor, exhibits an IC50 of 0.33 nM against its target and demonstrates broad-spectrum cytotoxicity against human cancer cell lines. Additionally, it inhibits MOLT3 cells with an IC50 of 2.1 μM [1].

FGFR1 inhibitor-9 (Compound 7) is an FGFR1 inhibitor with potent binding affinity, exhibiting an IC50 of 0.85 nM. It targets the ATP-binding pocket of FGFR1 and demonstrates anticancer activity [1].

FGFR1/DDR2 inhibitor 1 is an inhibitor of discoindin domain receptor 2 (DDR2) and fibroblast growth factor receptor 1 (FGFR1), with IC50 values of 31.1 nM, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.

FGFR1 inhibitor-8 (Compound 9), an FGFR1 inhibitor with an IC50 of 0.5 nM, binds to the ATP-binding pocket of FGFR1 and exhibits anticancer activity [1].

FGFR1 inhibitor-2 (with an IC50 of 4.55 μM in MDA-MB-231 cells) is a potent inhibitor of FGFR1. It is specifically useful for studying metastatic triple-negative breast cancer.

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.CAS 번호13460-73-81-1

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].

Irpagratinib (ABSK011) is an orally active fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor with specificity for FGFR4, exhibiting an IC50 of less than 10 nM. It effectively inhibits FGFR4 auto-phosphorylation and disrupts subsequent signal transduction to downstream pathways. Demonstrating high exposure in pharmacokinetic studies in mice, rats, and dogs, Irpagratinib also displays antineoplastic activity in subcutaneous xenograft tumor models [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].

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

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.

CE-245677 is a selective, orally active Tie2 kinase inhibitor identified by Pfizer previously in development for the treatment of certain cancers. CE-245,677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50 of 4.7 and 1 nM, resp., displays >100x selectivity against a number of other angiogenic receptor tyrosine kinases (e.g. KDR, PDGFR, FGFR) and gene family panels, and demonstrates good oral absorption in in vivo rat PK studies (F=80%).

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

Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor（KDR, Flt-1, FGFR1 and PDGFRα with IC50s of 4nM, 20nM, 4nM, 2 nM ,respectively）

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

FGFR-IN-7 (compound 17) is an orally active, potent FGFR modulator with the ability to penetrate the blood-brain barrier. It exhibits neuroprotective properties, enhancing brain exposure and decreasing the likelihood of phospholidosis. FGFR-IN-7 proves valuable for research on neurodegenerative diseases [1].

FGFR-IN-11 (compound I-5) is an orally active, covalent inhibitor of FGFR, exhibiting 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 proliferation of various cancer cells and significantly hinders tumor growth in xenograft mouse models [1].

FGFR-IN-3 (compound 6) is a highly potent and orally active modulator of FGFR (fibroblast growth factor receptor). It has the ability to penetrate the blood-brain barrier (BBB). Additionally, FGFR-IN-3 exhibits significant neuroprotective properties. Therefore, it holds potential for research on neurodegenerative diseases [1].

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.