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

FGFR

Fibroblast growth factor receptor

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-172921
    FGFR-IN-18
    Inhibitor
    FGFR-IN-18 (Compound KF7) is a lysine-targeting FGFR covalent inhibitor, with IC50s of: 1.1 nM for FGFR2, 1.3 nM for FGFR1, 31.5 nM for FGFR4. FGFR-IN-18 also has affinity for FGFR3 (inhibition rate of 52% at 10 nM). FGFR-IN-18 covalently modifies Lys485 (an reactive site of FGFRs).
    FGFR-IN-18
  • HY-E70719
    FGFR3 K650E Recombinant Human Active Protein Kinase
    FGFR3 activating mutations are drivers of malignancy in several human tissues, including bladder, lung, cervix, and blood. FGFR3 K650E is a mutant of FGFR3 that may be present in multiple myeloma cell lines. FGFR3 K650E Recombinant Human Active Protein Kinase is a recombinant FGFR3 K650E protein that can be used to study FGFR3 K650E-related functions.
    FGFR3 K650E Recombinant Human Active Protein Kinase
  • HY-143881
    FGFR4-IN-6
    Inhibitor
    FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity. FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    FGFR4-IN-6
  • HY-163569
    FGFR4-IN-20
    Inhibitor
    FGFR4-IN-20 (comp 11) is an orally active and selective FGFR4 inhibitor with IC50s of 19 and 36 nM against Huh7 cells and FGFR4 enzyme. FGFR4-IN-20 can be used for hepatocellular carcinoma research.
    FGFR4-IN-20
  • HY-172916
    LC-SF-14
    Inhibitor
    LC-SF-14 is a selective dual inhibitor of SHP2 and FGFR (IC50 values are 71.6 and 8.9 nM, respectively). LC-SF-14 inhibits FGFR2-FRS2α-SHP2-MAPK signaling and ERK phosphorylation. LC-SF-14 inhibits the proliferation of KATOIII cancer cells (IC50: 9.2 nM). LC-SF-14 has antitumor activity in the SNU-16 xenograft mouse model. LC-SF-14 can be used in FGFR2-driven gastric cancer research.
    LC-SF-14
  • HY-E70822
    FGFR2 N549H 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 N549H is a mutant of FGFR3. FGFR2 N549H Recombinant Human Active Protein Kinase is a recombinant FGFR4 N535H protein that can be used to study FGFR4 N535H-related functions.
    FGFR2 N549H Recombinant Human Active Protein Kinase
  • HY-158248
    FGFR4-IN-19
    Inhibitor
    FGFR4-IN-19 (compound 8B) is a potent covalent fibroblast growth factor receptor 4 (FGFR4) inhibitor (IC50=1.2 nM). FGFR4-IN-19 achieves high efficiency and isotype selectivity by covalently targeting a rare cysteine (C552) in the FGFR4 kinase domain. FGFR4-IN-19 can be used for hepatocellular carcinoma (HCC) research.
    FGFR4-IN-19
  • HY-177668
    Umedaptanib pegol
    Inhibitor
    Umedaptanib pegol is an anti-fibroblast growth factor-2 (FGF2) aptamer. It is used for the study of neovascular age-related macular degeneration (nAMD).
    Umedaptanib pegol
  • HY-172787
    FGFR4-IN-23
    Inhibitor
    FGFR4-IN-23 (compound 48c) is a FGFR4 inhibitor with an IC50 value of 2.9 nM against FGFR4WT kinase. FGFR4-IN-23 inhibits the phosphorylation of FGFR4, AKT and MAPK.
    FGFR4-IN-23
  • HY-150026
    Multi-kinase-IN-2
    Inhibitor
    Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity.
    Multi-kinase-IN-2
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity