2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. FGFR

FGFR

Fibroblast growth factor receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-149487
    FGFR1 inhibitor-8
    		Inhibitor
    FGFR1 inhibitor-8 (Compound 9) is a FGFR1 inhibitor (IC50s: 0.5 nM). FGFR1 inhibitor-8 binds to the ATP-binding pocket of FGFR1. FGFR1 inhibitor-8 has anticancer activity.
    FGFR1 inhibitor-8
  • HY-139996
    Pomalidomide-C5-Dovitinib
    		Inhibitor
    Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD+ acute myeloid leukemia.
    Pomalidomide-C5-Dovitinib
  • HY-161995
    FGFR1/VEGFR2-IN-2
    		Inhibitor
    FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells.
    FGFR1/VEGFR2-IN-2
  • HY-144759
    FGFR4-IN-9
    		Inhibitor
    FGFR4-IN-9 (Compound 6O) is a selective FGFR4 inhibitor with an IC50 of 75.3 nM. FGFR4-IN-9 effectively inhibits both the growth and angiogenesis of HCC.
    FGFR4-IN-9
  • HY-172251
    FGFR-IN-17
    		Inhibitor
    FGFR-IN-17 (Compound 12l) is an orally active irreversible inhibitor of FGFR, which has a strong inhibitory effect on FGFR and its mutants. FGFR-IN-17 can inhibit the proliferation and migration, and induce apoptosis of non-small cell lung cancer cells. FGFR-IN-17 has anti-tumor activity.
    FGFR-IN-17
  • HY-115902
    FGFR4-IN-7
    		Inhibitor
    FGFR4-IN-7 (Compound C3) is a covalent reversible FGFR4 inhibitor with an IC50 value of 0.42 μM. FGFR4-IN-7 induces apoptosis via the FGFR4 signaling pathway blockage. FGFR4-IN-7 can be used for the research of hepatocellular carcinoma (HCC).
    FGFR4-IN-7
  • HY-B0636S1
    Triamcinolone acetonide-13C3
    Triamcinolone acetonide-13C3 is the 13C-labeled Triamcinolone acetonide (HY-B0636). Triamcinolone acetonide inhibits basic fibroblast growth factor (bFGF) induced proliferation of retinal endothelial cells. Triamcinolone acetonide reduces chondrocyte viability and leads to cartilage destruction. Triamcinolone acetonide activates macrophage with anti-inflammatory characteristics. Triamcinolone acetonide can be used in the study of diseases such as atopic dermatitis.
    Triamcinolone acetonide-<sup>13</sup>C<sub>3</sub>
  • HY-N0060AR
    Ferulic acid sodium (Standard)
    		Inhibitor
    10-Deacetyltaxol (Standard) is the analytical standard of 10-Deacetyltaxol. This product is intended for research and analytical applications. 10-Deacetyltaxol (10-Deacetylpaclitaxel) is a taxane derivative isolated from Taxus wallichiana Zucc. 10-Deacetyltaxol (10-Deacetylpaclitaxel) promotes the polymerization of tubulin and to inhibit the depolymerization of microtubules induced by cold or by calcium ions in vitro. 10-Deacetyltaxol (10-Deacetylpaclitaxel) exhibits cytotoxicity in human glial and neuroblastoma cell-lines.
    Ferulic acid sodium (Standard)
  • HY-149415
    Multi-kinase-IN-5
    		Inhibitor
    Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC50 of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively.
    Multi-kinase-IN-5
  • HY-152146
    HDAC-IN-50
    		Inhibitor
    HDAC-IN-50 is a potent and orally active FGFR and HDAC dual inhibitor with IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity.
    HDAC-IN-50
  • HY-143272
    FGFR1 inhibitor-6
    		Inhibitor
    FGFR1 inhibitor-6 is a potent FGFR1 inhibitor with an IC50 value of 16.31 nM. FGFR1 inhibitor-6 shows cytotoxic activities. FGFR1 inhibitor-6 induces apoptosis and cell cycle arrest at pre-G1 and G2/M phase.
    FGFR1 inhibitor-6
  • HY-172922
    FGFR-IN-19
    		Inhibitor
    Arg-IN-1 is a selective Arginine (Arg)-targeting covalent inhibitor with IC50s of 9.7 nM and 30.4 nM for FGFR2 and FGFR3,respectively. Arg-IN-1 has the potential to avoid FGFR1/4-targeted toxicity as well as conquer acquired on-target resistance, potential for FGFR-targeting cancer therapy.
    FGFR-IN-19
  • HY-P5903
    FGF acidic I (102-111) (bovine brain)
    FGF acidic I (102-111) (bovine brain) (aFGF (102-111)) is the 102-111 fragment of acidic FGF that can be used as a potential neurotrophic agent.
    FGF acidic I (102-111) (bovine brain)
  • HY-16135A
    CEP-11981 tosylate
    		Inhibitor
    CEP-11981 (tosylate) (ESK981 (tosylate), BOL 303213X (tosylate)) is an orally active tyrosine kinase inhibitor (TKI), which can target TIE2, VEGFR1-3 and FGFR1, and has potential anti-tumor and anti-angiogenic effects.
    CEP-11981 tosylate
  • HY-E70820
    FGFR2 L617V Recombinant Human Active Protein Kinase
    FGFR2 is a receptor tyrosine kinase that is involved in many human cancers such as intrahepatic cholangiocarcinomas and hepatocellular carcinomas. FGFR2 L617V is a mutant of FGFR3. FGFR2 L617V Recombinant Human Active Protein Kinase is a recombinant FGFR2 L617V protein that can be used to study FGFR2 L617V-related functions.
    FGFR2 L617V Recombinant Human Active Protein Kinase
  • HY-170934
    BW710
    		Inhibitor
    BW710 is an orally active fibroblast growth factor receptor 2 (FGFR2) inhibitor. BW710 inhibits the proliferation of BaF3-FGFR2 cells with an IC50 of 2.8 nM. BW710 abolishes FGFR2 enzymatic activity and is selective against other 75 tyrosine kinases including FGFR1, FGFR3, and FGFR4 at 1 μM. BW710 suppresses the FGFR2 signaling and selectively inhibits FGFR2-driven cancer cell proliferation. BW710 displays reasonable pharmacokinetic properties with an oral bioavailability of 29 % in mice.
    BW710
  • HY-P3695A
    VSPPLTLGQLLS TFA
    		Inhibitor
    VSPPLTLGQLLS TFA is a small peptide FGFR3 inhibitor, peptide P3, inhibits FGFR3 phosphorylation. VSPPLTLGQLLS TFA inhibits 9-cisRA-induced tracheal lymphangiogenesis and blocks lymphatic endothelial cell (LEC) proliferation, migration, and tubule formation.
    VSPPLTLGQLLS TFA
  • HY-172923
    FGFR-IN-20
    		Inhibitor
    Glu-IN-1 (compound AF1) is a covalent and selective FGFR2 inhibitor with an IC50 of 1.6 μM. Glu-IN-1 covalently modifies Glu489 in FGFR2.
    FGFR-IN-20
  • HY-168286
    FGFR-IN-16
    		Inhibitor
    FGFR-IN-16 (compound 7N) is a potent inhibitor of FGFR1, FGFR2, and FGFR4, with the IC50s of 8 nM, 4 nM and 3.8 nM, respectively. FGFR-IN-16 plays an important role in cancer research1].
    FGFR-IN-16
  • HY-145836
    FGFR4-IN-8
    		Inhibitor
    FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4V550L, FGFR4V550M and FGFR4C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model.
    FGFR4-IN-8
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity