2. シグナル伝達
  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.

製品番号 製品名 製品効果 純度 構造式
  • 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-181005
    FGFR-IN-25 Inhibitor
    FGFR-IN-25 (Compound 19E) is a FGFR inhibitor (IC50s: 1.30 nM and 0.85 nM for FGFR1 and FGFR2, respectively) and radiosensitizer. FGFR-IN-25 effectively reduces the phosphorylation of FGFR1 and its key downstream effectors, pAKT and pERK. FGFR-IN-25 exerts broad-spectrum antitumor activity against gastric cancer, colorectal carcinoma, hepatocellular carcinoma, breast cancer, triple-negative breast cancer, and glioblastoma. FGFR-IN-25, when combined with radiotherapy, synergistically activates the ROS-Caspase-3-GSDME axis, downregulates PD-L1 expression, and induces immunogenic cell death (ICD). FGFR-IN-25 combined with radiotherapy improves the antitumor efficacy.
    FGFR-IN-25
  • 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
  • HY-162626
    PROTAC FGFR2 degrader 2 Degrader
    FGFR2 degrader 1 (compound 28E) is a selectively PROTACS degrader of FGFR2, with the DC50 of 0.645 nM. FGFR2 plays an important role in cancer research (Pink: ligand of target protein; (HY-13304) black: linker; blue: ligand of E3 ligase).
    PROTAC FGFR2 degrader 2
  • HY-E70718
    FGFR3 G697C Recombinant Human Active Protein Kinase
    FGFR3 activating mutations are drivers of malignancy in several human tissues, including bladder, lung, cervix, and blood. FGFR3 G697C is a mutant of FGFR3 that may be present in oral squamous cell carcinoma. FGFR3 G697C increases FGFR3 auto-phosphorylation. FGFR3 G697C Recombinant Human Active Protein Kinase is a recombinant FGFR3 G697C protein that can be used to study FGFR3 G697C-related functions.
    FGFR3 G697C Recombinant Human Active Protein Kinase
  • HY-E70821
    FGFR2 M537I 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 M537I is a mutant of FGFR3. FGFR2 M537I Recombinant Human Active Protein Kinase is a recombinant FGFR2 M537I protein that can be used to study FGFR2 M537I-related functions.
    FGFR2 M537I Recombinant Human Active Protein Kinase
  • HY-P992195
    Anti-Beta Klotho Antibody
    Anti-Beta Klotho Antibody is a monoclonal antibody targeting *Beta Klotho*. It can be used in ELISA, FACS, and functional assays. For isotype controls of Anti-Beta Klotho Antibody, please refer to Human IgG1 (L234A/L235A) kappa, Isotype Control (HY-P991207).
    Anti-Beta Klotho Antibody
  • HY-174974
    ISM7594 Inhibitor
    ISM7594 is an orally active FGFR2/3 inhibitor. ISM7594 shows broad-spectrum antiproliferative potency in FGFR2- or FGFR3-altered cancer cell panels, including FGFR2/3 amplification, fusion, and mutation (BaF3-TEL-FGFR2-V564F (IC50 = 0.067 nM), BaF3-TEL-FGFR2-V564I (IC50 = 2 nM)) types. ISM7594 inhibits tumor growth in a dose-dependent manner. ISM7594 can be used for the study of advanced solid tumors with FGFR2/3 aberrations.
    ISM7594
  • HY-149512
    FGFR1/VEGFR2-IN-1 Inhibitor
    FGFR1/VEGFR2-IN-1 (compound 2b) is an FGFR1/VEGFR2 inhibitor. FGFR1/VEGFR2-IN-1 can be used for cancer research.
    FGFR1/VEGFR2-IN-1
  • HY-E70824
    FGFR2 R612T 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 R612T is a mutant of FGFR3. FGFR2 R612T Recombinant Human Active Protein Kinase is a recombinant FGFR2 R612T protein that can be used to study FGFR2 R612T-related functions.
    FGFR2 R612T Recombinant Human Active Protein Kinase
  • HY-147715
    FGFR3-IN-3 Inhibitor
    FGFR3-IN-3 (compound 40a) is a potent and pan-FGFR inhibitor, with IC50s of 2.1 nM, 3.1 nM, 4.3 nM and 74 nM for FGFR1, 2, 3, and 4, respectively. FGFR3-IN-3 can be used for the research of bladder cancer.
    FGFR3-IN-3
  • HY-135605
    PNU-145156E Inhibitor
    PNU-145156E (FCE26644) is an angiogenesis inhibitor with anti-tumor activity. PNU-145156E inhibits the binding of bFGF to its receptor and inhibits bFGF-induced endothelial cell proliferation and motility.
    PNU-145156E
  • HY-147713
    FGFR3-IN-1 Inhibitor
    FGFR3-IN-1 (compound 1) is a fibroblast growth factor receptor (FGFR) inhibitor, with IC50s of 40 nM, 5.1 nM, and 12 nM for FGFR1, 2, and 3, respectively. FGFR3-IN-1 can be used for the research of bladder cancer.
    FGFR3-IN-1
  • HY-E70819
    FGFR2 K659N 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 K659N is a mutant of FGFR3. FGFR2 K659N Recombinant Human Active Protein Kinase is a recombinant FGFR2 K659N protein that can be used to study FGFR2 K659N-related functions.
    FGFR2 K659N Recombinant Human Active Protein Kinase
  • HY-122888
    MPT0L145 Inhibitor
    MPT0L145 is a PIK3C3/FGFR inhibitor, with a Kd value of 0.53 nM for PIK3C3. MPT0L145 decreases the phosphorylation of FGFR1, FGFR3 and their downstream proteins (FRS2, ERK and Akt). MPT0L145 induces G0/G1 cell cycle arrest and decreased protein levels of cyclin E. MPT0L145 promotes mitochondrial dysfunction, ROS production, and DNA damage. MPT0L145 is an autophagy inhibitor. MPT0L145 significantly sensitizes cancer cells to targeted or chemotherapeutic agents. MPT0L145 can be used for cancer research, such as bladder cancer and NSCLC.
    MPT0L145
  • HY-147684
    FGFR-IN-7 Modulator
    FGFR-IN-7 (compound 17) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-7 shows neuroprotective activity. FGFR-IN-7 improves brain exposure and reduced risk of phospholidosis. FGFR-IN-7 can be used for neurodegenerative diseases research.
    FGFR-IN-7
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