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-10331AR
    Regorafenib monohydrate (Standard)
    Inhibitor
    Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.
    Regorafenib monohydrate (Standard)
  • HY-W801893
    FGFR1 inhibitor-13
    Inhibitor
    FGFR1 inhibitor-13 (compound 1) is an FGFR1 inhibitor with an IC50 of 4.2 μM.
    FGFR1 inhibitor-13
  • HY-170776
    AXL/Angiokinase-IN-1
    Inhibitor
    AXL/Angiokinase-IN-1 (compound 11b) is an AXL/triple angiokinase inhibitor, IC50=3.75 nM (AXL expression). AXL/Angiokinase-IN-1 inhibits epithelial-mesenchymal transition (EMT) in Bxpc-3, blocking lung cancer cell metastasis. AXL/Angiokinase-IN-1 also inhibits vascular and fibroblast functions, promoting apoptosis (apoptosis) in cancer cells and fibroblasts. AXL/Angiokinase-IN-1 features low toxicity and good metabolic stability.
    AXL/Angiokinase-IN-1
  • HY-182915
    FGFR-IN-26
    Inhibitor
    FGFR-IN-26 is an orally active FGFR inhibitor. FGFR-IN-26 inhibits FGFR2 wild-type and clinically relevant resistance mutations. FGFR-IN-26 inhibits tumor growth in FGFR2-amplified xenograft mouse models. FGFR-IN-26 can be used for the research of cancer, suah as gastric carcinoma.
    FGFR-IN-26
  • HY-181031
    FGFR-IN-24
    Inhibitor
    FGFR-IN-24 (Compound 8r) is a FGFR inhibitor. FGFR-IN-24 potently inhibits FGFR1/2/3 with IC50 values of 10.0, 6.9, and 30.2 nM, respectively. FGFR-IN-24 exhibits superior inhibitory activity toward FGFR1V561M, FGFR2V564F, and FGFR2N549K mutations with IC50 values of 6.8, 0.7, and 0.8 nM, respectively. FGFR-IN-24 induces Apoptosis. FGFR-IN-24 efficiently suppresses the phosphorylation of FGFR2 and its downstream signaling mediators (AKT and MAPK). FGFR-IN-24 demonstrates favorable antitumor efficacy in an RT112/84 bladder cancer xenograft model.
    FGFR-IN-24
  • HY-158011
    FGFR3-IN-9
    Inhibitor
    FGFR3-IN-9 (example27) is a selective FGFR3 inhibitor.
    FGFR3-IN-9
  • HY-151903S
    FGFR2/3-IN-1
    Inhibitor
    FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively.
    FGFR2/3-IN-1
  • HY-176547
    FGFR2/3-IN-3
    Inhibitor
    FGFR2/3-IN-3 is a dual-target FGFR2/3 inhibitor with IC50s of 2.7 nM (TEL-FGFR2) and 3.9 nM (TEL-FGFR3), respectively. FGFR2/3-IN-3 has effective activity against both wild-type and mutant FGFR3. FGFR2/3-IN-3 has low CYP3A4 inhibitory effect and hERG toxicity. FGFR2/3-IN-3 improves the imbalance between chondrocyte proliferation and differentiation and promotes bone growth by inhibiting the signaling pathway mediated by mutant FGFR3. FGFR2/3-IN-3 shows a growth-promoting effect in a dwarfism mouse model and has the potential to study bone development disorder-related diseases such as achondroplasia (ACH).
    FGFR2/3-IN-3
  • HY-178059
    FGFR-IN-23
    Inhibitor
    FGFR-IN-23 (Compound 9p) is a covalent pan FGFR inhibitor with IC50s of 14, 4.2, 5 and 220 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. FGFR-IN-23 also has potent inhibitory activity against gatekeeper mutants, such as FGFR1V561M and FGFR3V555M. FGFR-IN-23 suppresses the activation of FGFR-mediated signaling and induces apoptosis. FGFR-IN-23 shows significant antitumor efficacy in RT112 xenograft mouse models. FGFR-IN-23 can be used for cancers and its drug resistance research.
    FGFR-IN-23
  • HY-153502
    FGFR4-IN-13
    Inhibitor
    FGFR4-IN-13 (Compound 6) is a selective FGFR4 inhibitor. FGFR4-IN-13 is applicable to the research of hepatocellular carcinoma.
    FGFR4-IN-13
  • HY-RS04923
    Fgfr4 Rat Pre-designed siRNA Set A
    Inhibitor

    Fgfr4 Rat Pre-designed siRNA Set A contains three designed siRNAs for Fgfr4 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Fgfr4 Rat Pre-designed siRNA Set A
  • HY-163620
    LHQ490
    Inhibitor
    LHQ490 is a selective FGFR2 inhibitor, with an IC50 of 5.2 nM. LHQ490 efficiently inhibits the proliferation of BaF3-FGFR2 cells with an IC50 value of 1.4 nM. LHQ490 inhibits FGFR2-driven cancer cell proliferation and induces apoptosis of FGFR2-driven cancer cells.
    LHQ490
  • HY-156704
    FGFR4-IN-16
    Inhibitor
    FGFR4-IN-16 (CY-15-2) is a covalent inhibitor of FGFR-4 for cancer research.
    FGFR4-IN-16
  • HY-162283
    FGFR4-IN-18
    Inhibitor
    FGFR4-IN-18 (compound 8z) is an inhibitor of FGFR4 and can be used in cancer research.
    FGFR4-IN-18
  • HY-161841
    Antitumor agent-177
    Inhibitor
    Antitumor agent-177 (compound 57), a non-steroidal NSC12 derivative, shows potent FGF2 binding affinity with a Kd of 24 μM by SPR. Antitumor agent-177 significantly inhibits the formation of HSPG/FGF2/FGFR1 ternary complexes. Antitumor agent-177 inhibits FGFR activation and exerts a potent anti-tumor activity on multiple myeloma (MM) cell lines in vitro and in vivo.
    Antitumor agent-177
  • HY-147620
    FGFR-IN-5
    Inhibitor
    FGFR-IN-5 is a potent inhibitor of FGFR. Fibroblast growth factor receptor (FGFR) is a tyrosine kinase receptor that binds to fibroblast growth factor ligands. FGFR-IN-5 has the potential for the research of cancer diseases (extracted from patent WO2022042612A1, compound 3). FGFR-IN-5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    FGFR-IN-5
  • HY-155028
    FGFR-IN-11
    Inhibitor
    FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models.
    FGFR-IN-11
  • HY-141685
    3-Methylthienyl-carbonyl-JNJ-7706621
    Inhibitor
    3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC50s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC50=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC50=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer.
    3-Methylthienyl-carbonyl-JNJ-7706621
  • HY-147793
    FGFR4-IN-12
    Inhibitor
    FGFR4-IN-12 (Compound A34) is a potent inhibitor of FGFR4. FGFR4-IN-12 exhibits improved FGFR4 inhibitory capability and selectivity and excellent anti-proliferative activities against FGFR4-dependent HCC cell lines. FGFR4-IN-12 has the potential for the research of cancer diseases. FGFR4-IN-12 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-12
  • HY-161840
    Antitumor agent-176
    Inhibitor
    Antitumor agent-176 (Compound 22), an antitumor agent, can effectively bind to FGF2 and inhibit the activation of fibroblast growth factor receptor (FGFR) in multiple myeloma (MM) cells, exhibiting significant antitumor activity both in vivo and in vitro against MM.
    Antitumor agent-176
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity