Signaling Pathway

FGFR

FGFR

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FGFR (Fibroblast growth factor receptors) are the receptors that bind to members of the fibroblast growth factor family of proteins. Some of these receptors are involved in pathological conditions. A point mutation in FGFR3 can lead to achondroplasia. Five distinct membrane FGFR have been identified in vertebrates and all of them belong to the tyrosine kinase superfamily (FGFR1, FGFR2, FGFR3, FGFR4, FGFR6). The fibroblast growth factor family constitutes one of the most important groups of paracrine factors that act during development. They are responsible for determining certain cells to become mesoderm, for the production of blood vessels, for limb outgrowth, and for the growth and differentiation of numerous cell types. As we study developmental biology, we will see fibroblast growth factors popping up all over the embryo.

FGFR Inhibitors & Modulators (25)

Product Name Catalog No. Brief Description
ACTB-1003

HY-16025

ACTB-1003 is a potent inhibitor of FGFR1 with IC50 <10 nM in FGFR-1 biochemical assay; more information can be find in Patent WO/2007/064883A2, Example 12.

AZD4547

HY-13330

AZD4547 is a novel selective FGFR inhibitor targeting FGFR1/2/3 with IC50 of 0.2 nM/2.5 nM/1.8 nM, weaker activity against FGFR4, VEGFR2(KDR), and little activity observed against IGFR, CDK2, and p38.

BIBF 1120

HY-50904

Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM.

BIBF 1120 esylate

HY-11106

Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM.

BIBF 1202

HY-15992

BIBF 1202 is the carboxylate metabolite of BIBF 1120, which is an oral triple angiokinase inhibitor targeting VEGFR, PDGFR, FGFR.

BLU-554

HY-100492

BLU-554 is a potent fibroblast growth factor receptor 4 (FGFR4) inhibitor.

BLU9931

HY-12823

BLU9931 is the first selective small molecule inhibitor of FGFR4 with IC50 of 3 nM; less potent for FGFR1/2/3(IC50> 150 nM).

CH5183284

HY-19957

CH5183284 is a selective and orally available FGFR1/2/3 inhibitor.

E-3810

HY-15391

E-3810 is a novel dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs) with antiangiogenic activity.

Erdafitinib

HY-18708

Erdafitinib is a quinoxaline derivative compound, acts on FGFR1/2/3/4 with mean pIC50 of ~ 9/8.5/8.5/8.25, respectively.

FGFR-IN-1

HY-100818

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

FGFR4-IN-1

HY-100631

FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM.

FIIN-2

HY-18602

FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively.

FIIN-3

HY-18603

FIIN-3 is an irreversible inhibitor of FGFR1-4 with IC50s of 13, 21, 31, and 35 nM, respectively.

Formononetin

HY-N0183

Formononetin (Formononetol; Flavosil) is a bioactive component extracted from the red clover; inhibits the proliferation of DU-145/PC-3 cells in a dose-dependent manner.

LY2874455

HY-13304

LY2874455 is a novel and potent FGF/FGFR inhibitor.

NVP-BGJ398

HY-13311

NVP-BGJ398(BGJ-398) 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.

NVP-BGJ398 phosphate

HY-13311A

NVP-BGJ398 phosphate (BGJ-398) 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.

PD173074

HY-10321

PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM, ~1000-fold selective for FGFR1 than PDGFR and c-Src.

Ponatinib

HY-12047

Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively.