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Fibroblast growth factor receptor (FGFR) inhibitors act on FGFR1 to FGFR4, four receptor tyrosine kinases. FGFR signaling controls cell proliferation, migration and differentiation in development and angiogenesis. Amplifications, activating mutations and gene fusions of FGFR genes have been found in many tumor types. PD173074 was crystallized with the FGFR1 kinase domain in 1998, which showed how it occupies the adenosine triphosphate (ATP) pocket. Infigratinib and fexagratinib are FGFR-focused inhibitors used to study cells that depend on FGFR signaling. Nintedanib and pazopanib HCl inhibit FGFR together with vascular endothelial growth factor receptors (VEGFRs) and platelet-derived growth factor receptors (PDGFRs). Kinases outside the FGFR family are covered by sibling categories such as VEGFR and PDGFR.
Synonyms: CH5183284; FF-284
Debio-1347 is an orally bioavailable inhibitor of the fibroblast growth factor receptor subtypes 1 (FGFR-1), 2 (FGFR-2) and 3 (FGFR-3), with potential antineoplastic activity.
Synonyms: ACTB1003
ACTB-1003 is an oral kinase inhibitor targeting cancer mutations (FGFR inhibition), angiogenesis (inhibition of VEGFR2 and Tie-2) and induces apoptosis (targeting RSK and p70S6K, downstream of PI3 kinase).
Synonyms: Lucitanib
E-3810 is a potent and selective dual inhibitor of VEGF and FGF receptors with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM and 82.5 nM for VEGFR-1, VEGFR-2, VEGFR-3, FGFR-1 and FGFR-2, respectively.
Synonyms: BGJ-398 phosphate
NVP-BGJ398 phosphate is a novel selective, pan-specific FGFR inhibitor with IC50 of 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively; >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes.
BLU9931 is the first selective small molecule inhibitor of FGFR4 with IC50 of 3 nM; less potent for FGFR1/2/3(IC50> 150 nM),
Synonyms: RPT-835
Alofanib is a potent and selective allosteric inhibitor of FGFR2 with potential anticancer activity.
Synonyms: JNJ 42756493
Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity.
FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM.
H3B-6527 is a highly selective FGFR4 inhibitor with potent antitumour activity in FGF19 amplified cell lines and mice.
Synonyms: ARQ087
Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT.
Synonyms: BAY-1163877
Rogaratinib, also known as BAY-1163877, is an aberrant fibroblast growth factor receptor (FGFR) inhibitor.
PD166866 is a FGFR1 inhibitor with IC50 value of 55 nM, and no effect on c-Src, PDGFR-b, EGFR or insulin receptor tyrosine kinases or MEK, PKC, and CDK4.
Synonyms: E7080 mesylate; E 7080
Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
FGFR1/DDR2 inhibitor 1 is an inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.
ODM-203 is a potent FGFR and VEGFR families inhibitor with IC50s of 11, 16, 6, 35 nM towards recombinant FGFR1, FGFR2, FGFR3 and FGFR4 as well as 26, 9, 5 nM towards VEGFR1, VEGFR2 and VEGFR3, respectively.
PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively.
Synonyms: FGF-401
Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity.
Heparan sulfate, a complex and linear polysaccharide, exists as part of glycoproteins named heparan sulfate proteoglycans, which are expressed abundantly on the cell surface and in the extracellular matrix.
Synonyms: INCB054828; INCB54828
Pemigatinib is a selective FGFR inhibitor in development for the treatment of patients with cholangiocarcinoma.
SUN11602 is a novel aniline compound with basic fibroblast growth factor-like activity.
Synonyms: BLU-554
Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM.
ASP5878 is an oral active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3, and 4 kinase activity. ASP5878 has potential antineoplastic activity.
PP58 is a pyrido[2,3-d]pyrimidine-based compound that inhibits PDGFR, FGFR and Src family activities with nanomolar IC50 values.
S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
Synonyms: KHS 101
KHS101 hydrochloride could selectively induce a neuronal differentiation phenotype and interacts with transforming acidic coiled-coil-containing protein 3 (TACC3).
