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-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-145425
    PAIR2
    		Activator
    PAIR2 is a highly selective inhibitor targeting the kinase domain of human IRE1α, with a Ki value of 8.8 nM against human IRE1α. PAIR2 fully occupies the ATP-binding site of the IRE1α kinase domain, partially antagonizes the ribonuclease activity of IRE1α, specifically inhibits regulated IRE1α-dependent decay (RIDD) and its mediated substrate cleavage, while preserving the splicing function of Xbp1 mRNA. PAIR2 also promotes the differentiation of B cells into plasma cells, blocks IRE1α-induced cell apoptosis, and restores the expression of Fgfr2 mRNA in AT2 cells. PAIR2 effectively reaches a steady-state concentration in the lung tissues of Mus musculus, and serves as an important tool for investigating the function of the IRE1α signaling pathway in diseases such as pulmonary fibrosis.
    PAIR2
  • 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-111289
    Tec-IN-14
    Tec-IN-14 blocks the interaction between Tec kinase and FGF2 with an IC50 of 7.0 μM. Tec-IN-14 inhibits the non-classical secretion of FGF2 in cells. Tec-IN-14 suppresses the tyrosine phosphorylation of FGF2 in a cellular environment. Tec-IN-14 is applicable to research related to cancer.
    Tec-IN-14
  • 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
  • HY-163527
    FGFR-IN-13
    		Inhibitor
    FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity.
    FGFR-IN-13
  • HY-172618
    FGFR1 inhibitor-18
    		Inhibitor
    FGFR1 inhibitor-18 (compound 16) is a potent FGFR1 inhibitor with an IC50 value of 1.31 nM. FGFR1 inhibitor-18 can occupy within the ATP-binding pocket of the target FGFR1.
    FGFR1 inhibitor-18
  • HY-10321G
    PD173074 (GMP)
    		Inhibitor
    PD173074 GMP is PD173074 (HY-10321) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. PD173074 is an orally active FGFR inhibitor that targets the transphosphorylation of FGFR1 and FGFR2 and blocks the FGF signaling pathway. By reducing the phosphorylation level of SMAD2 and altering the expression of Nodal/Activin target genes, PD173074 eliminates endothelial differentiation potential, thereby inhibiting the formation of capillary-like structures. PD173074 blocks the proliferation and colony formation of tumor cells and increases intratumoral cell apoptosis. PD173074 successfully reverses FGF-2-induced chemoresistance to enhance the effect of cisplatin (HY-17394) in small cell lung cancer models. PD173074 can be applied to research related to critical limb ischemia and small cell lung cancer.
    PD173074 (GMP)
  • HY-RS04921
    FGFR4 Human Pre-designed siRNA Set A
    		Inhibitor

    FGFR4 Human Pre-designed siRNA Set A contains three designed siRNAs for FGFR4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    FGFR4 Human Pre-designed siRNA Set A
  • HY-177276
    FGFR-IN-22
    		Inhibitor
    FGFR-IN-22 (Compound 23) is a FGFR inhibitor with IC50s of 0.631, 1.26, 0.851 and 1 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. FGFR-IN-22 effectively inhibits cell proliferation that depends on the FGFR1 and FGFR3 signaling pathway. FGFR-IN-22 can be used for cancers such as chronic lymphocytic leukemia (CLL) research.
    FGFR-IN-22
  • HY-181752
    FGFR3-IN-12
    		Inhibitor
    FGFR3-IN-12 is a selective fibroblast growth factor receptor 3 (FGFR3) inhibitor with an IC50 of 6.8 nM. FGFR3-IN-12 shows an IC50 of 19.2 nM against FGFR3V555M and an IC50 of 16.9 nM against TNK1 (Thirty-eight Negative Kinase 1). FGFR3-IN-12 inhibits cancer cells proliferation and induces caspase-mediated apoptosis. FGFR3-IN-12 exhibits antitumor activity in bladder cancer xenografts mice models. FGFR3-IN-12 can be used for the research of cancer, such as bladder cancer.
    FGFR3-IN-12
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity